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N-Phenylacrylamide is a special polymer showing highaffinity with Ochratoxin A, a colorless and crystalline mycotoxin compound. N-Phenylacrylamide can be applied in the field of mycotoxin extraction, and be used for the security research of agricultural commodities and foods made from cereals and grapes .
Cipralisant (GT-2331) enantiomer is the enantiomer of Cipralisant (HY-106993), Cipralisant is an orally active, potent, selective, and highaffinityhistamine H3 receptor antagonist (rat Ki=0.47 nM) . Cipralisant (enantiomer) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
IMP 245 is a symmetric di-HSG bivalent hapten. IMP 245 has low toxicity, highaffinity binding to available antibodies and absence of cross reactivity or non-specific binding with body components .
DCDAPH (Compound 2c) is a novel smart NIRF probe for detection of β-amyloid (Aβ) plaques (λex/λem=597/665 nm in PBS). DCDAPH shows highaffinity for Aβ aggregates (Ki=37 nM, Kd=27 nM). DCDAPH shows good blood brain barrier permeation and can meet most of the requirements for the detection of Aβ plaques both in vitro and in vivo .
AZD4694 Precursor (AZ13040214) is the precursor of [ 18F] AZD4694 for the synthesis of [ 18F] AZD4694, an amyloid-β imaging ligand with highaffinity for amyloid-β plaques .
FK888 is a potent, selective, and highaffinity dipeptide NK1 receptor antagonist. FK888 displaces [3H]-SP binding with a Ki value of 0.69 nM and 0.45 microM. FK888 also inhibits SP-induced airway oedema in guinea-pig after both intravenous and oral administration .
Dual FAAH/sEH-IN-1 (compound 3) is a highaffinity dual sEH (soluble epoxide hydrolase) and FAAH (fatty acid amide hydrolase) inhibitor, with IC50 values of 9.6 and 7 nM, respectively. Dual FAAH/sEH-IN-1 shows antinociception against the inflammatory phase .
SYL3C aptamer sodium is a DNA aptamer that targets the epithelial cell adhesion molecule (EpCAM) on the surface of cancer cells. SYL3C aptamer sodium targets multiple human cancer cell lines including MDA-MB-231, Kato III, HT-29, T47D and SW480. The Kd of SYL3C aptamer sodium against breast cancer cell line MDA-MB-231 and gastric cancer cell line Kato III is 38 nM and 67 nM, respectively. SYL3C aptamer sodium provides stability, high binding affinity, and selectivity for targeted cancer therapy, cancer cell imaging, and circulating tumor cell detection .
TAK-615 is a negative allosteric modulator (NAM) of the LPA1 receptor for the research of pulmonary fibrosis. TAK-615 binds the LPA1 receptor with highaffinity (Kdhighaffinity of 1.7 nM and Kd low affinity of 14.5 nM) .
GMT 4 aptamer sodium is a nucleic acid aptamer targeting different glioblastoma cell lines and exhibits highaffinity. GMT 4 aptamer sodium also shows high binding affinity to the T lymphocyte cell line CCRF-CEM .
GMT 8 aptamer sodium is a nucleic acid aptamer targeting different glioblastoma cell lines and exhibits highaffinity. GMT 4 aptamer sodium also shows high binding affinity to the T lymphocyte cell line CCRF-CEM .
BTSA1 is a potent, highaffinity and orally active BAX activator with an IC50 of 250 nM and an EC50 of 144 nM. BTSA1 binds with highaffinity and specificity to the N-terminal activation site and induces conformational changes to BAX leading to BAX-mediated apoptosis .
Endomorphin 2, a highaffinity, highly selective agonist of the μ-opioid receptor, displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM.
Acetalin-3 (Ac-RFMWMT-NH2), a hexapeptide, is a μ opioid receptor antagonist with highaffinity for μ and κ3 opioid receptor, weak affinity for κ1 receptors and no affinity for κ2 receptors .
Acetalin-1 (Ac-RFMWMK-NH2), a hexapeptide, is a μ opioid receptor antagonist with highaffinity for μ and κ3 opioid receptor, weak affinity for κ1 receptors and no affinity for κ2 receptors .
Endomorphin 2 TFA, a highaffinity, highly selective agonist of the μ-opioid receptor, displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM .
THK-5105, an arylquinoline derivative, displays high binding affinity to tau fibrils. THK-5105 has high binding affinity to tau protein aggregates and tau-rich Alzheimer disease (AD) brain homogenates. 18F-THK-5105 has the potential to act as a tau imaging PET probe .
Cligosiban (PF-3274167), a high oral bioavailability and good brain-penetrant non-peptide oxytocin receptor antagonist, shows a high-affinity (Ki=9.5 nM) and an excellent selectivity versus the vasopressin receptors with almost no affinity for the V1b and V1a subtypes. Cligosiban inhibits ejaculatory physiology in rodents .
4-IBP is a selective σ1 agonist, binding to σ1 receptors with highaffinity (Ki = 1.7 nM) and with slightly weaker affinity to σ2 receptors (Ki = 25.2 nM).
Talsupram (hydrochloride) is a selective norepinephrine inhibitor with highaffinity for norepinephrine transporter (NET) and can be used in the study of neuropathic pain .
Ph-HTBA is a high-affinity, brain-penetrating modulator for CaMKIIα. Ph-HTBA has binding affinity for CaMKIIα with a Kd value of 757 nM. Ph-HTBA can be used for the research of ischemia and neurodegenerative disorders .
Halo tag TMR is a fluorescent dye composed of Halo tag ligand molecules and TMR. Halo tag can rapidly form stable covalent binding with Halo protein with high specificity and highaffinity .
THK-5117, an arylquinoline derivative, displays high binding affinity to tau fibrils with a Ki of 10.5 nM. THK-5117 has high binding affinity to tau protein aggregates and tau-rich Alzheimer disease (AD) brain homogenates. 18F-THK-5117 has the potential to act as a tau imaging PET probe .
BRD4 D1-IN-1 is a selective BRD4 D1 inhibitor (IC50<0.092 µM). BRD4 D1-IN-1 has 18 nM affinity against BRD4 D1 and over 500-fold selectivity against BRD2 D1 and BRD4 D2 via ITC .
BRD4 D1-IN-2 (compound 26) is a potent and selective BRD4 D1 inhibitor (IC50<0.092 µM). BRD4 D1-IN-2 has 15 nM affinity against BRD4 D1 and over 500-fold selectivity against BRD2 D1 and BRD4 D2 via ITC .
NF-56-EJ40 is a potent, high-affinity, and highly selective human SUCNR1 (GPR91) antagonist with an IC50 of 25 nM and a Ki of 33 nM, and shows almost no activity towards rat SUCNR1. NF-56-EJ40 has highaffinity for humanized rat SUCNR1 with a Ki value of 17.4 nM .
Pridopidine, a dopamine (DA) stabilizer, acts as a low affinitydopamine D2 receptor (D2R) antagonist. Pridopidine exerts highaffinity towards sigma 1 receptor (S1R) with Ki between 70 and 80 nM, which is ~100× higher than its affinity toward D2R.
Afegostat is a pharmacological chaperone, which specifically and reversibly binds acid-β-glucosidase (GCase) in the endoplasmic reticulum (ER) with highaffinity .
FR167344 free base is an orally active, nonpeptide bradykinin receptor B2 antagonist. FR167344 free base shows a highaffinity binding to the B2 receptor with an IC50 value of 65 nM and no binding affinity for the B1 receptor.
Dihydroergotoxine mesylate is a complex of closely related alkaloid salts; Binds with highaffinity to the GABAA receptor Cl- channel, producing an allosteric interaction with the benzodiazepine site.
Neurotensin, a gut tridecapeptide, acts as a potent cellular mitogen for various colorectal and pancreatic cancers which possess high-affinityneurotensin receptors (NTR).
AHN 1-055 hydrochloride is a dopamine uptake inhibitor, with an IC50 of 71 nM. AHN 1-055 hydrochloride binds with highaffinity to the dopamine transporter (DAT) .
Fluticasone dimer impurity is a dimeric impurity of Fluticasone Propionate . Fluticasone propionate is a corticosteroid with comparatively high receptor affinity and topical activity .
Afegostat tartrate is a pharmacological chaperone, which specifically and reversibly binds acid-β-glucosidase (GCase) in the endoplasmic reticulum (ER) with highaffinity .
Afegostat D-Tartrate is a pharmacological chaperone, which specifically and reversibly binds acid-β-glucosidase (GCase) in the endoplasmic reticulum (ER) with highaffinity .
YQ456 is a novel small molecule inhibitor of myoferlin that showed high binding affinity to myoferlin with a KD of 37 nM and excellent anti-invasion capability with an IC50 of 110 nM.
Endomorphin 1, a highaffinity, highly selective agonist of the μ-opioid receptor (Ki: 1.11 nM), displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM. Endomorphin 1 has antinociceptive properties .
Mosapramine (Clospipramine) is an orally active and potent dopamine receptor antagonist with highaffinity to dopamine receptor subtypes 2, 3 and 4, and with moderate affinity for the 5-HT 2 receptor. Mosapramine shows antipsychotic activity and can be used in schizophrenia research .
Endomorphin 1 acetate, a highaffinity, highly selective agonist of the μ-opioid receptor (Ki: 1.11 nM), displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM. Endomorphin 1 acetate has antinociceptive properties .
Fluo-3FF pentapotassium is a cell-permeable acetoxy-methyl ester of Fluo-3FF, a fluorescent calcium indicator. Fluo-3FF is a di-fluorinated analog of Fluo-3 with a 100-fold lower affinity than Fluo-3 for calcium (Kds = 42 and 0.4 碌M, respectively). For its low affinity, Fluo-3FF is used for studying compartments with high concentrations of calcium, such as endoplasmic reticulum, where highaffinity dyes will be insensitive to luminal fluctuations.
Cariprazine is a novel antipsychotic agent candidate that exhibits highaffinity for the D3 (Ki=0.085 nM) and D2 (Ki=0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (Ki=2.6 nM).
Cariprazine hydrochloride is a novel antipsychotic agent candidate that exhibits highaffinity for the D3 (Ki=0.085 nM) and D2 (Ki=0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (Ki=2.6 nM).
Galanin-Like Peptide (porcine) is a 60 amino acid neuropeptide that was first isolated from the porcine hypothalamus. Galanin-Like Peptide (porcine) has a highaffinity for the GALR2 receptor (IC50 of 0.24 nM) and a lower affinity for the GALR1 receptor (IC50 of 4.3 nM) .
Inolitazone dihydrochloride (Efatutazone dihydrochloride) is a novel high-affinityPPARγ agonist that is dependent upon PPARγ for its biological activity with IC50 of 0.8 nM for growth inhibition.
Dexetimide ((+)-Benzetimide; (S)-(+)-Dexetimide; Dexbenzetimide) is a piperidine anticholinergic and a high-affinitymuscarinic receptor antagonist. Dexetimide can be used in studies of parkinson's disease .
TASP0390325 is a highaffinity and orally active arginine vasopressin receptor 1B (V1B receptor) antagonist with antidepressant and anxiolytic activities .
Calcipotriol (Standard) is the analytical standard of Calcipotriol. This product is intended for research and analytical applications. Calcipotriol is a synthetic VitD3 analogue with a highaffinity for the vitamin D receptor.
Cutamesine (SA4503; AGY-94806) is a selective sigma 1 receptor(σ1R) agonist; highaffinity for the sigma 1 receptor (IC50= 17.4±1.9 nM); 100-fold less affinity for the sigma 2 receptor.
BMS CCR2 22 is a potent, specific and highaffinityCC-type chemokine receptor 2 (CCR2) antagonist with excellent binding affinity (binding IC50 of 5.1 nM) and potent functional antagonism (calcium flux IC50 of 18 nM and chemotaxis IC50 of 1 nM) .
4F 4PP (oxalate) is a selective 5-HT2A antagonist with almost as highaffinity (Ki= 5.3 nM) as ketanserin but with a much lower affinity for 5-HT2C sites (Ki= 620 nM) .
DN02 is a potent, selective BRD8 bromodomain probe. DN02 has exhibits highaffinity for the BRD8(1) (Ki=32 nM), which is 30-fold more affinity than BRD8 (2) (Ki>1000 nM) .
SCH 221510 is a potent, orally active and selective NOP (nociceptin opioid receptor) agonist, with an EC50 of 12 nM and Ki of 0.3 nM. SCH 221510 shows an anxiolytic-like effect .
AM3102 is an oleoylethanolamide (OEA) analog. AM3102 is an endogenous high-affinity PPAR-alpha agonist. AM3102 resists enzymatic hydrolysis, activates PPAR-alpha with high potency in vitro, and persistently reduces feeding when administered in vivo either parenterally or orally .
NBI-98782 is a highaffinity and selectivity vesicular monoamine transporter 2 (VMAT2) inhibitor with a Ki of 3 nM. NBI-98782 has antipsychotic activity .
Oleoylethanolamide-d2 is the deuterium labeled Oleoylethanolamide. Oleoylethanolamide is a highaffinity endogenous PPAR-α agonist, which plays an important role in the treatment of obesity and arteriosclerosis.
Oleoylethanolamide-d4 is the deuterium labeled Oleoylethanolamide. Oleoylethanolamide is a highaffinity endogenous PPAR-α agonist, which plays an important role in the treatment of obesity and arteriosclerosis.
Fura-FF pentapotassium is a low-affinity fluorescent dye for calcium (Ex/Em: 365/514 nm in the absence of calcium; 339/507 nm in the presence of a high calcium concentration) .
TAMRA-isoADPr is a fluorescently tagged iso-ADP-ribose tracer compound. TAMRA-isoADPr is a high-affinity tracer for the RNF146 WWE domain with a Kd of 45.2 nM .
Desmethyl cariprazine is an active metabolite of Cariprazine . Cariprazine, an antipsychotic agent candidate, exhibits highaffinity for the D3 (Ki=0.085 nM) and D2 (0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (2.6 nM) .
Cariprazine-d6 is a deuterium labeled Cariprazine. Cariprazine Cariprazine is an antipsychotic agent that exhibits highaffinity for the D3 (Ki of 0.085 nM) and D2 (Ki of 0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (Ki of 2.6 nM)[1].
Pipamperone (Floropipamide; McN-JR 3345) dihydrochloride is a high-affinity antagonist of 5-HT2A receptor (pKi=8.2) and D4 receptor (pKi=8.0) and a low-affinity antagonist of D2 receptor (pKi=6.7) .
Panamesine (EMD 57445) is a sigma receptor ligand, which has a highaffinity (IC50 6 nM) and selectivity for sigma binding sites. Panamesine is a potential atypical neuroleptic agent .
DIPPA (hydrochloride) is an irreversible, long-lasting, selective and highaffinityκ-opioid receptor antagonist. DIPPA (hydrochloride) can be used for the research of anxiety and antidepressant .
Acifran (AY 25712), an antihyperlipidemic agent, is an orally active agonist of GPR109A (HM74A) and GPR109B, the high and low affinity receptors for Niacin .
Ambenonium (WIN 8077) chloride is an orally active and reversible inhibitor of Acetyicholinesterase (AChE) with highaffinity. Ambenonium chloride inhibits human AChE with an IC50 value of 0.7 nM (hAChE) .
Stellasterol is a natural product. Stellasterol has highaffinity towards Bcl-2 protein (Ki: 118.05 nM). Stellasterol is a weak α-glucosidase inhibitor .
SR16835 has highaffinity for both NOPr and MOPr, with full agonist activity for NOPr and partial agonist activity for MOPr. SR16835 has no analgesic effect .
RS 23597-190 (EP-A-501322) is a highaffinity and selective 5-HT4 receptor antagonist. RS 23597-190 inhibits 5-HT-induced tachycardia. RS 23597-190 significantly inhibits superoxide production in high glucose .
BP 897 hydrochloride is a potent and partial dopamine D3 receptor agonist and a weak D2 receptor antagonist. BP 897 hydrochloride displays a highaffinity at the dopamine D3 receptor (Ki=0.92 nM) and a 70 times lower affinity at the D2 receptor (Ki=61 nM) .
BP 897 is a potent and partial dopamine D3 receptor agonist and a weak D2 receptor antagonist. BP 897 displays a highaffinity at the dopamine D3 receptor (Ki=0.92 nM) and a 70 times lower affinity at the D2 receptor (Ki=61 nM) .
PG 116800 (PG 530742) is an orally avtive MMP inhibitor. PG 116800 has highaffinity for MMP-2, -3, -8, -9, -13, and -14, while having substantially lower affinity for MMP-1 and -7. PG 116800 can be used for knee osteoarthritis research .
Bromperidol (R-11333) possesses antipsychotic activity, with a highaffinity for central dopamine receptors D2. Bromperidol can kill Mycobacteria in a synergistic manner with Spectinomycin .
Dansylcadaverine (Monodansyl cadaverine) is an autofluorescent compound used for the labeling of autophagic vacuoles. Dansylcadaverine, a highaffinity substrate of transglutaminases, can block the receptor-mediated endocytosis of many ligands .
EC0489, a conjugate of folic acid and desacetyl vinblastine hydrazide, is a high-affinity ligand for the folate receptor (FR). Refractory or metastatic Tumor . Small molecule-agent conjugate (SMDC) .
Harmine Hydrochloride (Telepathine Hydrochloride) is a natural DYRK inhibitor with anticancer and anti-inflammatory activities. Harmine has a highaffinity of 5-HT2A serotonin receptor, with an Ki of 397 nM .
Iodophenpropit dihydrobromide is a potent and selective histamine H3 receptor antagonist. The binding of [ 125I]Iodophenpropit is selective, saturable, readily reversible, and of highaffinity (KD 0.32 nM) .
Dazucorilant (CORT113176) is a selective and highaffinity non-steroidal glucocorticoid receptor (GR) modulator with a Ki value <1 nM in vitro. Dazucorilant can be used for the research of neurological disorders .
Bromperidol (R-11333) hydrochloride possesses antipsychotic activity, with a highaffinity for central dopamine receptors D2. Bromperidol hydrochloride can kill Mycobacteria in a synergistic manner with Spectinomycin .
Clozapine-d8 is the deuterium labeled Clozapine. Clozapine is an antipsychotic used for the research of schizophrenia. Clozapine has highaffinity for a number of neuroreceptors[1][2][3][4].
Carlumab (CNTO 888) is a human anti-CCL2 (chemokine ligand 2) antibody with highaffinity. Carlumab can be used in cancer research, particularly in prostate cancer .
preQ1 dihydrochloride is a modified, guanine-derived nucleobase and a precursor of Queuine (HY-N10574) biosynthesis. preQ1 dihydrochloride binds to the aptamer of PreQ1 riboswitch with highaffinity .
JNJ-40255293 is a high-affinity human A 2A receptor antagonist with a KiKi of 7.5 nM. JNJ-40255293 can be used in the research of neurodegenerative diseases such as Parkinson's disease .
Bosutinib isomer is a ligand or inhibitor with high binding affinity for both Wee1 and Wee2, with Kd values of 43.7 ± 10.0 and 4.7 ± 2.3 nM, respectively .
Aprepitant (Standard) is the analytical standard of Aprepitant. This product is intended for research and analytical applications. Aprepitant (MK-0869) is a selective and high-affinityneurokinin 1 receptor antagonist with a Kd of 86 pM.
Pipamperone (Floropipamide; McN-JR 3345; R 3345) is a high-affinity antagonist of 5-HT2A receptor (pKi=8.2) and D4 receptor (pKi=8.0) and a low-affinity antagonist of D2 receptor (pKi=6.7) .
SNAP 94847 hydrochloride is a novel, highaffinity selective melanin-concentrating hormonereceptor1 (MCHR1) antagonist with (Ki= 2.2 nM, Kd=530 pM), it displays >80-fold and >500-fold selectivity over MCHα1A and MCHD2 receptors respectively. SNAP 94847 hydrochloride binds with highaffinity to the mouse and rat MCHR1 with minimal cross-reactivity to other GPCR, ion channels, enzymes, and transporters .
SNAP 94847 is a novel, highaffinity selective melanin-concentrating hormonereceptor1 (MCHR1) antagonist with (Ki= 2.2 nM, Kd=530 pM), it displays >80-fold and >500-fold selectivity over MCHα1A and MCHD2 receptors respectively. SNAP 94847 binds with highaffinity to the mouse and rat MCHR1 with minimal cross-reactivity to other GPCR, ion channels, enzymes, and transporters .
Didesmethyl cariprazine is a metabolite of Cariprazine and acts as the predominant circulating active moiety. Didesmethyl cariprazine has a long half-life of 1-3 weeks. Cariprazine is a antipsychotic agent candidate that exhibits highaffinity for the D3 and D2 receptors, and moderate affinity for the 5-HT1A receptor .
Cariprazine-d8 is a deuterium labeled Cariprazine. Cariprazine is a novel antipsychotic agent candidate that exhibits highaffinity for the D3 (Ki=0.085 nM) and D2 (Ki=0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (Ki=2.6 nM).
Nestoron (ST-1435) is a 19-norprogesterone derivative with highaffinity and selectivity for progesterone receptors. Nestoron is a highly selective and potent progestogen that can be used as a hormonal contraceptive .
Travoprost (Fluprostenol isopropyl ester), an isopropyl ester proagent, is a highaffinity, selective FP prostaglandin full receptor agonist. Travoprost has the ocular hypotensive efficacy and has the potential for glaucoma and ocular hypertension .
KF21213 is a highly selective ligand for mapping CNS adenosine A2A receptors. KF21213 shows a highaffinity for the adenosine A2A receptors (Ki=3.0 nM).
Amylin, amide, rat is a potent and highaffinity ligand of Amylin receptor AMY1 and AMY3 receptors and variably of AMY2 receptors; binding studies are generally used for the latter receptor.
α-Zearalenol is a Mycotoxin with highaffinity for the estrogen receptors (ER),
α-Zearalenol is the derivative of zearalenone (ZEN), causes reproductive disorders in animals, due to its xenoestrogenic effects .
Odapipam (NNC 756) is a selective, highaffinity and benzazepine dopamine D1 receptor antagonist with a Kd of 0.18 nM. Odapipam is also a superior positron emission tomography (PET) radiotracer .
RO5203648 is a potent and highly selective partial agonist of TAAR1 (Trace amine-associated receptor 1) with highaffinity. RO5203648 demonstrates a novel paradigm for neuropsychiatric research .
Clozapine-d4 is the deuterium labeled Clozapine. Clozapine is an antipsychotic used for the research of schizophrenia. Clozapine has highaffinity for a number of neuroreceptors[1][2][3][4][5].
CP-601932 ((1S,5R)-CP-601927) is a high-affinity partial agonist at α3β4 nAChR (Ki=21 nM; EC50=~ 3 μM). CP-601932 has the same high-binding affinity at α4β2 nAChR (Ki=21 nM) and an order of magnitude lower affinity for α6 and α7 nAChR subtypes. CP-601932 selectively decreases ethanol but not sucrose consumption and operant self-administration following long-term exposure. CP-601932 can penetrate the CNS .
GSK256066 Trifluoroacetate is a selective and high-affinityphosphodiesterase 4 (PDE) inhibitor, with an IC50 of 3.2 pM for PDE4B. GSK256066 Trifluoroacetate is developed for the research of chronic obstructive pulmonary disease .
LY2444296 is an orally bioavailable, high-affinity and selective short-acting kappa opioid receptor (KOPR) antagonist, with a Ki value of ∼1 nM. LY2444296 exhibits anti-anxiety like effects .
MLS000532223 is a highaffinity, selective inhibitor of Rho family GTPases, with EC50 values ranging from 16 μM to 120 μM. MLS000532223 prevents GTP binding to several GTPases .
SJM-3 is a positive allosteric modulator of different isoforms of the GABAA receptor. SJM-3 binds at the high-affinity benzodiazepine binding site at the α+/γ- subunit interface .
CRANAD-2 is a near-infrared (NIR) Aβ plaque-specific fluorescent probe. CRANAD 2 penetrates the blood brain barrier and has a highaffinity for Aβ aggregates with a Kd of 38 nM .
ABP688 is a highaffinityhuman mGluR5 antagonist with anKi of 1.7 nM. Radioisotope-labeled ABP688 can be used as a PET tracer for clinical imaging of the mGlu5 receptor .
Namilumab (AMG203) is a human IgG1 monoclonal antibody that binds with highaffinity to the GM-CSF ligand, potently neutralizing GM-CSF. Namilumab can be used for the research of rheumatoid arthritis .
FAP Ligand 1 (FL), a high-affinity FAP small-molecule ligand, is used to target attached drugs to FAP-expressing fibroblasts and can be used in radiation imaging studies of targeted cancers .
GSK 1562590 hydrochloride is a highaffinity and selective antagonist of urotensin-II receptor (UT), with pKis of 9.14-9.66 for mammalian recombinant (mouse, rat, cat, monkey, human) and native UT .
Rovunaptabin (ARC 183) is a DNA aptamer, which is a single-stranded DNA molecule consisting of 15 deoxynucleotides that forms well-defined three-dimensional configuration, allowing it to bind to thrombin with highaffinity and specificity.
Ch55 is a potent synthetic retinoid. Ch55 binds to RAR-α and RAR-β receptors with highaffinity. Ch55 displays low affinity for cellular retinoic acid binding protein (CRABP). Ch55 is a potent inducer of the differentiation of HL60 cells with an EC50 of 200 nM. Ch55 can be used for cancer research .
RNA Aptamer Mango Ⅱ (sodium) has an exceptionally highaffinity to TO1-biotin (a thiazole orange derivative fluorophore), and can be used to visualize RNA expression or localization in live cells. Compared to the original Mango I aptamer, RNA Aptamer Mango Ⅱ (sodium) has markedly improved fluorescent properties, binding affinities, and salt dependencies.
RNA Aptamer Mango Ⅳ (sodium) has an exceptionally highaffinity to TO1-biotin (a thiazole orange derivative fluorophore), and can be used to visualize RNA expression or localization in live cells. Compared to the original Mango I aptamer, RNA Aptamer Mango Ⅳ has markedly improved fluorescent properties, binding affinities, and salt dependencies.
RNA Aptamer Mango Ⅲ (sodium) has an exceptionally highaffinity to TO1-biotin (a thiazole orange derivative fluorophore), and can be used to visualize RNA expression or localization in live cells. Compared to the original Mango I aptamer, RNA Aptamer Mango Ⅲ has markedly improved fluorescent properties, binding affinities, and salt dependencies.
(S)-Terazosin is an active S-enantiomer of Terazosin. (S)-Terazosin is a potent and high-affinityα-adrenoceptor antagonist with Ki values of 3.91 nM, 0.79 nM and 1.16 nM for α1a, α1b and α1d-adrenoceptor, respectively. (S)-Terazosin also has high-affinity for α2a, α2B and α2c-adrenoceptor with Ki values of 729 nM, 3.5 nM and 46.4 nM, respectively .
GSK256066 is a selective and high-affinityphosphodiesterase 4 (PDE4) inhibitor, with an IC50 of 3.2 pM for PDE4B. GSK256066 is developed for the research of chronic obstructive pulmonary disease .
MK-6892 is a potent, selective, and full agonist for the highaffinity nicotinic acid (NA) receptor GPR109A. Ki and GTPγS EC50 of MK-6892 on the Human GPR109A is 4 nM and 16 nM, respectively.
Crocetin (Transcrocetin), extracted from saffron (Crocus sativus L.), acts as an NMDA receptor antagonist with highaffinity . Crocetin is capable of crossing the blood-brain barrier and reach the central nervous system (CNS) .
A 1120 is a high-affinity nonretinoid retinol-binding protein 4 (RBP4) antagonist with a Ki value of 8.3 nM. A 1120 disrupts the interaction between RBP4 and its binding partner transthyretin .
Ambenonium (WIN 8077) dichloride tetrahydrate is an orally active and reversible inhibitor of Acetyicholinesterase (AChE) with highaffinity. Ambenonium dichloride tetrahydrate inhibits human AChE with an IC50 value of 0.7 nM (hAChE) .
ZnAF-2, 6-iso- is a cell-impermeable compound that acts as a high-affinity Zn2 -specific fluorescent probe (Kd = 2.7 nM). It exhibits low basal fluorescence with an approximately 51-fold increase in fluorescence intensity upon stoichiometric (1:1) binding to Zn2 . Little affinity for Ca2 , Mg2 , Na or K .
N-type calcium channel blocker-1 is an orally active compound which shows highaffinity to functionally block N-type calcium channels with an IC50 of 0.7 μM in the IMR32 assay.
Perzinfotel (EAA-090) is a potent, selective, and competitive NMDA receptor antagonist with neuroprotective effects. Perzinfotel (EAA-090) shows highaffinity (IC50=30 nM) for the glutamate site .
Lidoflazine is a highaffinity blocker of the HERG (human ether-a-go-go-related gene) K + channel. Lidoflazine is an antianginal calcium channel blocker that carries a significant risk of QT interval prolongation and ventricular arrhythmia .
JNJ-46281222 is an metabotropic glutamate (mGlu) 2-selective, highly potent PAM (positive allosteric modulator) with nanomolar affinity (Kd = 1.7 nM) and a high modulatory potency (pEC50 = 7.71) .
Nitrobenzylthioinosine is an ENT1 transporter inhibitor that binds to ENT1 transporter with highaffinity. Nitrobenzylthioinosine is a photoaffinity probe for adenosine uptake sites in brain. Nitrobenzylthioinosine can cross the blood-brain barrier .
(±)-Vesamicol hydrochloride ((±)-AH5183 hydrochloride) is a potent vesicular acetylcholine transport inhibitor with a Ki of 2 nM. (±)-Vesamicol hydrochloride also displays highaffinity for σ1 and σ2 receptors with Kis of 26 nM and 34 nM, respectively .
YM-298198 hydrochloride is a high-affinity, selective, orally active, and non-competitive antagonist of metabotropic glutamate receptor type 1 (mGluR1). YM-298198 hydrochloride can be used for the research of neurological disorders .
FSHR agonist 1 is a highaffinity and allosteric follicle stimulating hormone receptor (FSHR) agonist with a pEC50 of 7.72. FSHR agonist 1 formes extensive interactions with the TMD to directly activate FSHR .
RLH-033 is a potent and selective ligand for the sigma 1 recognition site. RLH-033 has highaffinity for sigma 1 sites labeled by [ 3H](+)-pentazocine with a Ki of 50 pM .
A 85380 hydrochloride is a novel, highaffinity neuronal nicotinic acetylcholine receptor (nAChR) agonist. A 85380 hydrochloride exhibits selectivity for the α4β2 nAChR subtypes. A 85380 hydrochloride has a broad-spectrum analgesic profile .
Camrelizumab (SHR-1210) is a potent humanied high-affinity IgG4-κ monoclonal antibody (mAb) to PD-1. Camrelizumab binds PD-1 at a highaffinity of 3 nM and inhibits the binding interaction of PD-1 and PD-L1 with an IC50 of 0.70 nM. Camrelizumab acts as anti-PD-1/PD-L1 agent and can be used for cancer research, including NSCLC, ESCC, Hodgkin lymphoma, and advanced HCC et,al .
GSK1324726A is a novel, potent, and selective inhibitor of BET proteins with highaffinity to BRD2 (IC50=41 nM), BRD3 (IC50=31 nM), and BRD4 (IC50=22 nM).
SB 258719 is a selective 5-HT7 receptor antagonist with highaffinity (pKi=7.5) for the receptor. SB 258719 can be used for the research of cancer and neurological disease .
L 888607 is a potent, selective, stable and orally active CRTH2 agonist. L 888607 has highaffinity for the human CRTH2 receptor with a Ki value of 4 nM. L 888607 can be used for the research of several physiological events and metabolite .
CB2 receptor agonist 2 is a potent and selective agonist for the CB2 (cannabinoid type 2) receptor with a Ki of 8.5 nM. CB2 receptor agonist 2 has highaffinity and selectivity for CB2 .
JNJ-42253432 is a CNS-penetrant, high-affinity and orally active P2X7 antagonist, with pKi values of 9.1 and 7.9 for rat and human P2X7 channels, respectively .
L-760735 is a highaffinity, selective and orally active NK1 receptor antagonist with an IC50 of 0.19 nM for human NK1 receptors. L-760735 exhibits anxiolytic and antidepressant-like effects .
Urocortin III (mouse) (free acid) is a selective CRF2 receptor agonist (with highaffinity for the CRF2 receptor). Urocortin III (mouse) (free acid) significantly inhibits gastric emptying without modifying colonic transit .
Harmine is a natural dual-specificity tyrosine phosphorylation-regulated kinase (DYRK) inhibitor with anticancer and anti-inflammatory activities. Harmine has a highaffinity of 5-HT2A serotonin receptor, with an Ki of 397 nM .
Camoteskimab (AVTX-007) is a fully human, high-affinity anti-IL-18 monoclonal antibody. Camoteskimab has the potential for the autoinflammatory diseases research, including adult-onset Still’s disease (AOSD) .
DOTA-NOC (DOTA-Nal3-octreotide) is a high-affinity ligand of somatostatin receptor subtypes 2, 3 and 5. DOTA-NOC can be used for labeling with various radiometals, and development of radiopeptide imaging .
4-Methylhistamine (hydrochloride) is a potent, highaffinity H4 receptor agonist Ki of 7 nM. 4-Methylhistamine (hydrochloride) displays more than 100-fold selectivity over other human histamine receptor subtypes .
Estradiol 17-(β-D-Glucuronide), a metabolite of estrogen, is well known to cause intrahepatic cholestasis in humans. Estradiol 17-(β-D-Glucuronide) is a high-affinity substrate for oatp organic anion transporter .
10-Cl-BBQ is a highaffinity AhR ligand with immunosuppressive activity. 10-Cl-BBQ promotes cytosol to nuclear translocation of AhR and activates the AhR-regulated reporter gene at nanomolar concentrations .
YQA14 is a highaffinity dopamine D3 receptor antagonist. YQA14 is anti-opioid addiction agent. YQA14 inhibits Morphine/Cocaine-induced conditioned place preference (CPP) in animals .
Aztreonam (lysine) is a monocyclic beta-lactam antibiotic, and has a very highaffinity for penicillin-binding protein 3 (PBP-3). Aztreonam (lysine) is active against Gram-negative aerobic bacteria .
AlF-PD-FAPI has affinity for FAP , with the IC50 of 0.13 nM, and shows a specific uptake, high internalized fraction, and low cellular efflux in vitro. AlF-PD-FAPI can be used as FAP-targeting tracer .
CCZ01048 TFA, a α-MSH analogue, exhibits high binding affinity to melanocortin 1 receptor (MC1R) with a Ki of 0.31 nM. CCZ01048 TFA shows rapid internalization into B16F10 melanoma cells and high in vivo stability. CCZ01048 TFA is a promising candidate for PET imaging of malignant melanoma .
U92016A hydrochloride is a potent, metabolically stable, orally acitive 5-HT1A receptor agonist with an exceptionally high degree of intrinsic activity . U92016A hydrochloride binds with highaffinity to human 5-HT1A receptors expressed in Chinese hamster ovary cells (Ki=0.2 nM) .
Trospium chloride is an orally active, specific and competitive antagonist of muscarinic cholinergic receptors (mAChRs), with antimuscarinic activity. Trospium chloride binds to muscarinic receptors M1, M2 and M3 with highaffinity, but not nicotinic, cholinergic receptors .
SW033291 is a potent and high-affinity inhibitor of 15-PGDH with a Ki of 0.1 nM. SW033291 increases prostaglandin PGE2 levels in bone marrow and other tissues. SW033291 also promotes tissue regeneration .
AB-MECA is a highaffinityA3 adenosine receptor agonist with a binding Ki of 430.5 nM for human A3 receptors in CHO cells. AB-MECA can enhance plasma histamine level .
RO1138452 is a potent and selective IP (prostacyclin) receptor antagonist. RO1138452 displays highaffinity for IP receptors. In human platelets, pKi is 9.3±0.1; in a recombinant IP receptor system, pKi is 8.7±0.06.
OTS964 is an orally active, highaffinity and selective TOPK inhibitor with an IC50 of 28 nM . OTS964 is also a potent inhibitor of the cyclin-dependent kinase CDK11, which binds to CDK11B with a Kd of 40 nM .
Y1R probe-1 (Compound 39) is a high-affinity fluorescence probe for the Neuropeptide Y Y1 Receptor. Y1R probe-1 has the potential for the research of cancer disease .
S26948 is a specific peroxisome proliferator-activated receptor γ (PPARγ) modulator (EC50=8.83 nM) with potent antidiabetes and antiatherogenic effects. S26948 is a specific high-affinity agonist for PPARγ .
LEO 134310 is a selective, non-steroidal glucocorticoid receptor (GR) agonist optimized for topical research., LEO 134310 showed highaffinity (EC50 of 14 nM) in a GR binding assay. LEO 134310 can be used for skin diseases .
Ravulizumab (ALXN1210) is a humanized monoclonal antibody that specifically binds with highaffinity to the human complement protein C5. Ravulizumab can be used for the research of paroxysmal nocturnal hemoglobinuria, atypical hemolytic uremic syndrome, and myasthenia gravis .
Axatilimab (SNDX-6352) is a humanized IgG4 antibody with highaffinity to CSF-1R. Axatilimab can be used for the research of chronic graft versus host disease (cGVHD) and neoplastic diseases .
PSMA-IN-3 (compound 17) is a novel high-affinityPSMA inhibitor with an IC50 value of 13 nM. PSMA-IN-3 is suitable for developing an 18F-labeled radioligand for PET imaging of PSMA in prostate cancer .
Desmethyl-YM-298198 hydrochloride is a high-affinity, selective, and noncompetitive mGluR1 antagonist (IC50: 16 nM). Desmethyl-YM-298198 hydrochloride has analgesic effect in Streptozotocin (HY-13753)-induced hyperalgesic mice .
Tebanicline, an analogue of epibatidine, is a neuronal nicotinic acetylcholine receptor agonist. Tebanicline exhibits potent antinociceptive effects and has a highaffinity for the α4β2 neuronal nicotinic acetylcholine receptor subunit in the central nervous system.
MMC(TMZ)-TOC has high binding affinity and selectivity for somatostatin receptor subtype-2 (SSTR2). MMC(TMZ)-TOC targets delivery of TMZ to SSTR2-positive tumor cells .
Bexarotene (LGD1069) is a high-affinity and selective retinoid X receptors (RXR) agonist with EC50s of 33, 24, 25 nM for RXRα, RXRβ, and RXRγ, respectively. Bexarotene shows limited affinity for RAR receptors (EC50 >10000 nM) . Bexarotene can be used for the research of cutaneous T-cell lymphoma.
Alcaftadine (R89674) is a histamine H1 receptor antagonist, which is used to prevent eye irritation brought on by allergic conjunctivitis. Alcaftadine is a broad-spectrum antihistamine displaying a highaffinity for histamine H1 and H2 receptors and a lower affinity for H4 receptors. Alcaftadine also exhibits modulatory action on immune cell recruitment and mast cell stabilizing effects .
WDR5-IN-5 is an orally active and selective inhibitor of WIN site of WD repeat domain 5 (WDR5). WDR5-IN-5 exhibits anti-proliferative activity towards cancer cells and good pharmacokinetics profile in mice. WDR5-IN-5 shows highaffinity to WDR5 and the binding affinity Ki value <0.02 nM .
α-Conotoxin SIA is a selective nicotinic acetylcholine receptor (nAChR) antagonist with highaffinity for the muscle nAChR. α-Conotoxin SIA preferentially targets the α/δ interface of the muscle nAChR in mouse muscle. In contrast, for Torpedo nAChR, α-Conotoxin SIA has a much higher affinity for the α/γ than for the α/δ interface .
LDV-FITC, a fluorescent peptide, is a FITC-conjugated LDV peptide (HY-P2267). LDV-FITC binds to the α4β1 integrin with highaffinity (Kd: 0.3 nM and 12 nM for binding to U937 cells in the presence and absence of Mn 2+ respectively). LDV-FITC can be used to detect α4β1 integrin affinity .
Fluo-3 AM is a fluorecent Ca 2+ chelator, with highaffinity for calcium. Fluo-3 AM can specifically identify intracellular calcium ions, with high sensitivity, low cytotoxicity, increased AM acetylmethyl ester can enter the cell well, after being sheared by the intracellular esterase stay in the cell to bind to calcium ions, produce strong fluorescence .
CCZ01048, a α-melanocyte-stimulating hormone (α-MSH) analogue, exhibits high binding affinity to melanocortin 1 receptor (MC1R) with a Ki of 0.31 nM. CCZ01048 shows rapid internalization into B16F10 melanoma cells and high in vivo stability. CCZ01048 is a promising candidate for PET imaging of malignant melanoma .
QM-FN-SO3 is a BBB-penetrable near-infrared (NIR) aggregation-induced emission (AIE)-active probe for Aβ plaques. QM-FN-SO3 can be used for in vivo detection of Aβ plaques. QM-FN-SO3 has ultra-high S/N ratio, binding affinity, and high-performance NIR emission .
LY2795050 is a short-acting selective κκ-opioid receptor (KOR) antagonist. LY2795050 has highaffinity for the KOR with Ki value of 0.72 nM. LY2795050 can be used for the research of central nervous system dysfunction .
Verubecestat (MK-8931) is an orally active, high-affinityBACE1 and BACE2 inhibitor with Ki values of 2.2 nM and 0.38 nM. Verubecestat effectively reduces Aβ40 and has the potential for Alzheimer's Disease .
Pancreatic Polypeptide, bovine, a 36-amino acid, straight chain polypeptide derived primarily from the pancreas, inhibits secretin- and cholecystokinin-stimulated pancreatic secretion; Pancreatic Polypeptide, bovine acts as an agonist of NPY receptor, with highaffinity at NPYR4.
p5 Ligand for Dnak and DnaJ is a nonapeptide, which corresponds to the main binding site for the 23-residue part of the presequence of mitochondrial aspartate aminotransferase. p5 Ligand for Dnak and DnaJ is a high-affinity ligand for DnaK and DnaJ .
β-Endorphin, equine TFA is an endogenous opioid peptide, which binds at highaffinity to both μ/δ opioid receptors. β-Endorphin, equine TFA has analgesic properties .
TBOPP is a selective inhibitor of DOCK1 with an IC50 of 8.4 μM. TBOPP binds to the DOCK1 DHR-2 domain with highaffinity (Kd of 7.1 μM), has anti-tumor activity for broader types of tumors .
Fasitibant chloride hydrochloride (MEN16132) is a potent, selective, highaffinity, and long-lasting nonpeptide bradykinin B2 (BK2) receptor antagonist. Fasitibant chloride hydrochloride has proinflammatory effects and can be used for the research of osteoarthritis and rheumatoid arthritis .
Aztreonam-d6 is deuterium labeled Aztreonam. Aztreonam (SQ-26,776) is a synthetic monocyclic beta-lactam antibiotic, which has a very highaffinity for penicillin-binding protein 3 (PBP-3).
Tralokinumab, a fully human IgG4 monoclonal antibody, specifically binds with highaffinity to IL-13 alone, preventing its interaction with the receptor and subsequent downstream signalling. Tralokinumab can be used for the research of the atopic dermatitis (AD) .
Mibefradil dihydrochloride hydrate (Ro 40-5967 dihydrochloride hydrate) is a effectively long-acting calcium channel antagonist, used as an antihypertensive agent. Mibefradil dihydrochloride hydrate acts via a higher affinity block for low-voltage-activated (T) than for high-voltage-activated (L) calcium channels .
PSB-0788 is a new selective high-affinityA2B antagonist with IC50 value of 3.64 nM and Ki value of 0.393 nM, respeactively. PSB-0788 can be used for the research for chronic inflammatory lung diseases .
Fasitibant (free base) is a potent, selective, highaffinity, and long-lasting nonpeptide bradykinin B2 (BK2) receptor antagonist. Fasitibant (free base) has proinflammatory effects and can be used for the research of osteoarthritis and rheumatoid arthritis .
GSK215083 is a highaffinity5-HT6 receptor antagonist. GSK215083 can serves as a promising 5-HT6 radioligand candidate by radiolabeled with (11)C via methylation .
PB131 is a selective and brain-permeable HDAC6 inhibitor with high binding affinity (IC50: 1.8 nM). PB131 has potent anti-inflammatory activity. PB131 can be used for research of inflammation, especially neuroinflammation .
S-14671 is a high-affinity5-HT1A agonist (pKi=9.3). S-14671 can be used for research on neurological diseases, such as anti-anxiety, anti-depression, etc .
Dicamba-propionic acid (DCa3) is a heterologous hapten that can be used to develop high-affinity monoclonal antibodies (mAb) against Dicamba. The Dicamba-propionic acid- developed mAb can be used to determine the residual amount of Dicamba in environmental water samples .
Oxomemazine is a phenothiazine-based histamine H1-receptor blocker with pronounced antimuscarinic properties. Oxomemazine is a selective antagonist for muscarinic M1 receptor, displays about 20-fold difference in the affinity for high (Ki = 84 nM, M1 receptor) and low (Ki = 1.65 μM, M2 receptor) affinity sites . Oxomemazine an antihistamine and anticholinergic agent used for the study of cough treatment .
Quin-2AM is a fluorecent Ca 2+ chelator, with highaffinity for calcium. Quin-2AM can specifically identify intracellular calcium ions, with high sensitivity, low cytotoxicity, increased AM acetylmethyl ester can enter the cell well, after being sheared by the intracellular esterase stay in the cell to bind to calcium ions, produce strong fluorescence .
8-Azanebularine, a compound with hydrogen in place of the C6 amino group, inhibits the ADAR2 reaction at high concentrations (IC50=15 mM). 8-Azanebularine is incorporated into an RNA structure recognized by human ADAR2 results in high-affinity binding (KD=2 nM). 8-Azanebularine can be used for the research of ADAR-catalyzed RNA-editing reaction .
Mag-Fluo-4 AM is a fluorecent Ca 2+ chelator, with highaffinity for calcium. Mag-Fluo-4 AM can specifically identify intracellular calcium ions, with high sensitivity, low cytotoxicity, increased AM acetylmethyl ester can enter the cell well, after being sheared by the intracellular esterase stay in the cell to bind to calcium ions, produce strong fluorescence .
Emedastine is an orally active, selective and highaffinityhistamine H1 receptor antagonist with a Ki value of 1.3 nM. Emedastine is a benzimidazole derivative with potent antiallergic properties and used for allergic rhinitis, allergic skin diseases and allergic conjunctivitis .
PSB-0739 is a high-affinity potent, competitive, nonselective platelet P2Y12 receptor antagonist with a Ki values of 24.9 nM. The P2Y12 receptor plays a crucial role in platelet aggregation. Antithrombotic effect .
Fluo-4FF AM is a cell-permeant fluorescent calcium indicator. Fluo-4FF is an analog of Fluo-4 with a lower affinity for calcium, which is suitable for investigation of relatively high level of intracellular calcium.
S0859 is a selective, high-affinity generic Na +/HCO3- transporter (NBC) inhibitor. S0859 reversibly inhibits NBC-mediated intracellular pH (pHi) recovery (Ki=1.7 μM, full inhibition at approximately 30 μM).
GSK484 hydrochloride is a selective and reversible peptidylarginine deiminase 4 (PAD4) inhibitor. GSK484 hydrochloride demonstrates highaffinity binding to PAD4 with IC50s of 50 nM in the absence of Calcium. In the presence of 2 mM Calcium, notably lower potency (250 nM) is observed.
SYM 2081 is a high-affinity ligand and potent, selective agonist of kainate receptors, inhibits [ 3H]-kainate binding with an IC50 of 35 nM, almost 3000- and 200-fold selectivity for kainate receptors over AMPA and NMDA receptors respectively .
EMPA is a high-affinity, reversible and selective orexin OX2 receptor antagonist. [ 3H]EMPA binds to human and rat OX2-HEK293 membranes with KD values of 1.1 and 1.4 nM respectively .
(-)-Isocorypalmine (Tetrahydrocolumbamine), isolated from the crude base fraction of Corydalis chaerophylla, is a dopamine receptor ligand . Recombinant CYP719A21 displays strict substrate specificity and highaffinity (Km=4.63 ± 0.71 μM) for (-)-Isocorypalmine .
NSC 625987 is a specific and high-affinityCDK4 inhibitor with an IC50 of 0.2 μM for CDK4:cyclin D1. NSC 625987 shows >500-fold selectivity for CDK4 over CDK2 .
Dopamine D3 receptor ligand is a potent, selective and highaffinity ligand for Dopamine D3 receptor with 89-fold selective for D3 over D2 (D3Ki= 8 nM, D2Ki= 715 nM) .
Epi-cryptoacetalide is a natural diterpenoid. Epi-cryptoacetalide reveals highaffinity to ER-α and PGE2 receptor (EP2 subtype) with Ki values of 0.3 μM and 1.92 μM, respectively. Epi-cryptoacetalide has anti-endometriosis activities .
RNA Aptamer Mango Ⅰ (sodium) consists of 39 nucleotides and has an exceptionally highaffinity to TO1-biotin (a thiazole orange derivative fluorophore). RNA Aptamer Mango Ⅰ (sodium) can be used to visualize RNA expression or localization in live cells.
RNA Aptamer Peach Ⅰ (sodium) has an exceptionally highaffinity to TO3-Biotin (TO3-B, red channel, ex: 637 nm, em: 658 nm), and can be used to visualize RNA expression or localization in live cells.
RNA Aptamer Peach Ⅱ (sodium) has an exceptionally highaffinity to TO3-Biotin (TO3-B, red channel, ex: 637 nm, em: 658 nm), and can be used to visualize RNA expression or localization in live cells.
α-Conotoxin GI has highaffinity for nAChR.α-Conotoxin GI is a short peptide toxin that can be isolated from the venom of Conus geographus.α-Conotoxin GI has the similar activity with neuromuscular blocking agent .
Verubecestat (MK-8931) TFA is an orally active, high-affinityBACE1 and BACE2 inhibitor with Ki values of 2.2 nM and 0.38 nM. Verubecestat TFA effectively reduces Aβ40 and has the potential for Alzheimer's Disease .
CRTh2 antagonist 4 (compound 58) is an inhibitor (IC50: 212 nM) of TH2 lymphocyte (CRTH2 or DP2) receptor with high binding affinity (Ki= 37 nM). CRTh2 antagonist 4 can be used in the study of severe allergic diseases .
Ro 64-6198 is a potent, selective, nonpeptide, high-affinity, high cellular permeability and brain penetration N/OFQ receptor (NOP) agonist with an EC50 value of 25.6 nM. Ro 64-6198 is at least 100 times more selective for the NOP receptor over the classic opioid receptors. Ro 64-6198 can be used for stress and anxiety, addiction, neuropathic pain, cough, and anorexia .
QM-FN-SO3 ammonium is a BBB-penetrable near-infrared (NIR) aggregation-induced emission (AIE)-active probe for Aβ plaques. QM-FN-SO3 ammonium can be used for in vivo detection of Aβ plaques. QM-FN-SO3 ammonium has ultra-high S/N ratio, binding affinity, and high-performance NIR emission .
AVE 0991 sodium salt is a nonpeptide and orally active Ang-(1-7) receptor Mas agonist. AVE 0991 competes for high-affinity binding of [ 125I]-Ang-(1-7) to bovine aortic endothelial cell membranes with IC50 of 21 nM .
S961 is an high-affinity and selective insulin receptor (IR) antagonist with IC50s of 0.048, 0.027, and 630 nM for HIR-A, HIR-B, and human insulin-like growth factor I receptor (HIGF-IR) in SPA-assay, respectively .
O-2050 is a highaffinitycannabinoid CB1 receptor antagonist with a Ki of 2.5 nM. O-2050 inhibits cannabinoid CB2 receptor (Ki=0.2 nM). O-2050 can cause locomotor stimulation in mice .
Kresoxim-methyl (BAS 490 F), a Strobilurin-based fungicide, inhibits the respiration at the complex III (cytochrome bc1 complex). Kresoxim-methyl binds to complex III from yeast with an apparent Kd of 0.07 μM proving a highaffinity for this enzyme .
Emedastine difumarate is an orally active, selective and highaffinityhistamine H1 receptor antagonist with a Ki value of 1.3 nM. Emedastine difumarate is a benzimidazole derivative with potent antiallergic properties and used for allergic rhinitis, allergic skin diseases and allergic conjunctivitis .
SNX-482, a peptidyl toxin of the spider Hysterocrates gigas, is a potent, highaffinity, selective and voltage-dependent R-type CaV2.3 channel blocker with an IC50 of 30 nM. SNX-482 has antinociceptive effect .
S961 acetate is an high-affinity and selective insulin receptor (IR) antagonist with IC50s of 0.048, 0.027, and 630 nM for HIR-A, HIR-B, and human insulin-like growth factor I receptor (HIGF-IR) in SPA-assay, respectively .
PF-3882845 is a remarkably highaffinity selective and orally efficacious mineralocorticoid receptor (MR binding IC50=2.7 nM) antagonist for hypertension and nephropathy. PF-3882845 also binds to progesterone receptor (PR) with the binding IC50 of 310 nM .
MRS2279 is a selective and highaffinityP2Y1 receptor antagonist, with a Ki of 2.5 nM and an IC50 of 51.6 nM. MRS2279 competitively inhibits ADP-promoted platelet aggregation with an apparent affnity (pKB=8.05) .
Secukinumab (AIN457) is a highaffinity, human monoclonal antibody targeted against interleukin (IL)-17A. Secukinumab is the first-in-class anti-IL-17 agent used for the research of plaque psoriasis, ankylosing spondylitis and psoriatic arthritis .
Felcisetrag (TD-8954) is an orally active, potent and selective 5-HT4 receptor agonist with gastrointestinal prokinetic properties. Felcisetrag has highaffinity (pKi =9.4) for human 5-HT4(c) receptors.
Thio-ITP (6-Thioinosine 5′-triphosphate) is an RNA polymerase activity competitive inhibitor. Thio-ITP has a high apparent affinity for the polymerases (RNA polymerase I Ki: 40.9 μM; RNA polymerase II Ki: 38.0 μM) .
Fresolimumab (GC1008) is a high-affinity fully human monoclonal antibody that neutralizes the active form of human TGFβ1, TGFβ2, and TGFβ3. Fresolimumab can be used for the research of cancer and fibrotic diseases .
A3AR antagonist 1 (compound 17) is a potent and selective human A3 adenosine receptor (AR) antagonist, with an Ki of 4.63 nM. A3AR antagonist 1 shows no affinity for the rat A3 AR even at high concentrations .
Acridine homodimer (NSC 219743), acridine dimer, is a fluorescence dye. Acridine homodimer emits a blue-green fluorescence when bound to DNA. Acridine homodimer has extremely highaffinity for AT-rich regions of nucleic acids, can be used for chromosome banding .
Abelacimab (MAA868) is a fully human IgG1 monoclonal antibody that binds with highaffinity to the catalytic structural domain of FXI and locks it in the zymogen conformation, thereby preventing its activation by FXIIa or thrombin. Abelacimab can be used in thromboembolic disease studies .
SARS-CoV-2-IN-50 (Compound X77C) is a SARS-CoV-2 main protease (M Pro) inhibitor.. SARS-CoV-2-IN-50 has a highaffinity to the catalytic site of M Pro .
Bromperidol (Standard) is the analytical standard of Bromperidol. This product is intended for research and analytical applications. Bromperidol (R-11333) possesses antipsychotic activity, with a highaffinity for central dopamine receptors D2. Bromperidol can kill Mycobacteria in a synergistic manner with Spectinomycin .
RXR antagonist 6 (Compound 33) is a highly selective RXR agonist, with EC50s of 9 nM, 18 nM, and 11 nM for RXRα, RXRβ, and RXRγ, respectively. RXR antagonist 6 binds to RXR with highaffinity (Kd = 0.03 μM) .
Tafluprost acid (AFP-172), an active metabolic form of Tafluprost, is a selective prostanoid FP receptor agonist. Tafluprost acid shows a highaffinity for human prostanoid FP receptor with Ki and EC50 values of 0.4 nM and 0.53 nM, respectively. Tafluprost acid has 126 times weaker binding affinity for prostanoid EP3 receptor (IC50=67 nM) than for the prostanoid FP receptor. Tafluprost acid can be used in the research of glaucoma .
KSK68 is a high-affinity dual sigma-1 and histamine H3 receptor antagonist, with Kis of 7.7, 3.6, 22.4 nM for H3 receptor, sigma-1, sigma-2 receptor respectively. KSK68 has negligible affinity at the other histamine receptor subtypes. KSK68 can be used for research of nociceptive and neuropathic pain .
MI-773 is a potent MDM2-p53 protein‐protein interaction (PPI) inhibitor with high binding affinity against MDM2 (Kd=8.2 nM). MI-773 has antitumor activity .
AZ876 is a potent and high-affinityLXR agonist. AZ876 displays 25-fold and 2.5-fold more potent than GW3965 (HY-10627) on human (h)LXRα and hLXRβ respectively .
Stattic is a potent STAT3 inhibitor and inhibits STAT3 phosphorylation (at Y705 and S727) . Stattic inhibits the binding of a highaffinity phosphopeptide for the SH2 domain of STAT3 . Stattic ameliorates the renal dysfunction in Alport syndrome (AS) mice .
5-HT1A modulator 1 displays very highaffinities for the 5HT1A, adrenergic α1 and dopamine D2 receptor with IC50s of 2 ±0.3 nM, 10 ± 3 nM and 40 ±9 nM, respectively.
LNP023 hydrochloride is an orally bioavailable, highly potent and highly selective factor B inhibitor. LNP023 shows direct, reversible, and high-affinity binding to human factor B with a KD of 7.9 nM. LNP023 inhibits factor B with an IC50 value of 10 nM .
Nelonicline (ABT-126) is an orally active and selective α7 nicotinic receptor agonist with highaffinity to α7 nAChRs in human brain (Ki=12.3 nM). Nelonicline is used for the research of shizophrenia and Alzheimer's disease .
Flesinoxan is a hypotensive agent and a potent, highaffinity and selective 5-hydroxytryptamine1A (5-HT1A) receptor agonist with an EC50 value of 24 nM. Flesinoxan also has effective anxiolytic/antidepressant effects .
S961 TFA is an high-affinity and selective insulin receptor (IR) antagonist with IC50s of 0.048, 0.027, and 630 nM for HIR-A, HIR-B, and human insulin-like growth factor I receptor (HIGF-IR) in SPA-assay, respectively .
GIP (1-30) amide, porcine is a full glucose-dependent insulinotropic polypeptide (GIP) receptor agonist with highaffinity equal to native GIP(1-42) . GIP (1-30) amide, porcine is a weak inhibitor of gastric acid secretion and potent stimulator of insulin.
Tetrabenazine Metabolite is an active metabolite of Tetrabenazine. Tetrabenazine Metabolite is a vesicular monoamine transporter 2 (VMAT2) inhibitor with a highaffinity (Ki=13.4 nM) . Tetrabenazine Metabolite is be developed for the treatment of chorea associated with Huntington’s disease and other hyperkinetic disorders .
cis-ACBD is a potent and selective inhibitor of the high-affinity, Na +-dependent plasma membrane glutamate transporter. cis-ACBD is a glutamate reuptake inhibitor. cis-ACBD also acts as linear competitive inhibitor of the uptake of D-[3H]aspartate .
Phenosafranine is a phenazine dye. Phenosafranine has high binding affinity to triplex RNA compared to the parent duplex form, binds through intercalation to both forms of RNA. Phenosafranine can be used for staining plant cells, determination of hemoglobin, dopamine, serotonin and so on .
CC-90002 is a humanized anti-CD47 monoclonal antibody (mAb). CC-90002 has a highaffinity for binding to CD47 with a subnanomolar Kd value. CC-90002 can be used for the research of hematologic malignancies and solid tumors .
Farletuzumab (MORAb-003) is a potent folate receptor-alpha (FRα) inhibitor. Farletuzumab is a humanized monoclonal antibody with highaffinity for FRα. Farletuzumab possesses growth-inhibitory functions on cells overexpressing FRα. Farletuzumab can be used in research of cancer .
Pozelimab (REGN3918) is a fully human IgG4 anti-C5 monoclonal antibody. Pozelimab binds to C5 and C5 variants with highaffinity and blocks complement-mediated hemolysis. Pozelimab can be used for the research of complement-mediated diseases .
MEN 11270, a cyclic decapeptide, is a B2 kinin receptor antagonist. MEN 11270 bound with high-affinity to the B2 kinin receptor constitutively expressed by WI38 human fibroblasts, inhibiting 3H-bradykinin (BK) with a pKi value of 10.3 .
(1S)-CCR2 antagonist 1 is a left-handed chiral body of CCR2 antagonist 1 (HY-112792). CCR2 antagonist 1 is a high-affinity and long-residence-time CCR2 antagonist, with a Ki of 2.4 nM .
Travoprost (Standard) is the analytical standard of Travoprost. This product is intended for research and analytical applications. Travoprost (Fluprostenol isopropyl ester), an isopropyl ester proagent, is a highaffinity, selective FP prostaglandin full receptor agonist. Travoprost has the ocular hypotensive efficacy and has the potential for glaucoma and ocular hypertension .
CD63-1 aptamer sodium is a high-affinity and specific DNA aptamer targeting the CD63 protein (Kd: 38.71 nM). CD63-1 aptamer sodium efficiently binds to CD63-positive cells, including breast cancer MDA-MB-231 cells and CD63-overexpressing HEK293T cells, with moderate binding affinity (Kd~100 nM) as assessed by flow cytometry .
CD63-2 aptamer sodium is a high-affinity and specific DNA aptamer targeting the CD63 protein (Kd: 78.43 nM). CD63-1 aptamer sodium efficiently binds to CD63-positive cells, including breast cancer MDA-MB-231 cells and CD63-overexpressing HEK293T cells, with moderate binding affinity (Kd~100 nM) as assessed by flow cytometry .
EM127 (compound 11c) is a SMYD3 covalent inhibitor with high selectivity, highaffinity (KD=13 μM) and site-specificity. EM127 effectively inhibits ERK1/2 phosphorylation and reduces transcriptional regulation of SMYD3 target genes. EM127 effectively and prolongedly impairs methyltransferase activity. EM127 can be used in cancer research, particularly in SMYD3 positive tumours .
Cabergoline is an ergot derived-dopamine D2-like receptor agonist that has highaffinity for D2, D3, and 5-HT2B receptors (Ki=0.7, 1.5, and 1.2, respectively).
Galanin Receptor Ligand M35 is a high-affinity ligand and antagonist of galanin receptor (Kd=0.1 nM). Galanin Receptor Ligand M35 exerts a Ki values of 0.11 and 2.0 nM for human galanin receptor type 1 and 2, respectively .
Iobenguane sulfate (MIBG sulfate) is an analogue of the neurotransmitter norepinephrine with antitumor activity. Radioiodinated Iobenguane sulfate is clinically used as a tumor-targeted radiopharmaceutical in the diagnosis and treatment of adrenergic tumors. Iobenguane sulfate is a high-affinity substrate for cholera toxin that interferes with cellular mono(ADP-ribosylation) .
p-MPPI hydrochloride is a selective 5-HT1A receptor antagonist with highaffinity for 5-HT1A receptors. p-MPPI hydrochloride can crosses the blood-brain barrier, and has clear antidepressant and anxiolytic-like effects .
F1324 acetate is a potent, highaffinity peptidic inhibitor of B cell lymphoma 6 (BCL6), with an IC50 of 1 nM. F1324 acetate exhibits binding t1/2 value of 441 s and has strong inhibition activity against BCL6 PPI .
F1324 is a potent, highaffinity peptidic inhibitor of B cell lymphoma 6 (BCL6) with an IC50 of 1 nM. F1324 exhibits binding t1/2 value of 441 s and has strong inhibition activity against BCL6 PPI .
GIP (1-30) amide, porcine TFA is a full glucose-dependent insulinotropic polypeptide (GIP) receptor agonist with highaffinity equal to native GIP(1-42) . GIP (1-30) amide, porcine is a weak inhibitor of gastric acid secretion and potent stimulator of insulin.
Cemsidomide (CFT7455) is an orally active zinc finger transcription factors Ikaros (IKZF1), Aiolos (IKZF3) degrader. Cemsidomide is an anti-cancer agent that binds with highaffinity to the cereblon E3 ligase (Kd of 0.9 nM) (WO2022032132A1; Compound 1) .
MRS2279 diammonium is a selective and highaffinityP2Y1 receptor antagonist, with a Ki value of 2.5 nM and an IC50 value of 51.6 nM. MRS2279 diammonium competitively inhibits ADP-promoted platelet aggregation with an pKb value of 8.05 .
Narsoplimab (OMS 721) is a high-affinity fully human immunoglobulin gamma 4 (IgG4) monoclonal antibody that binds MASP-2 and blocks lectin pathway activation. Narsoplimab can be used in research of hematopoietic stem-cell transplantation and SARS-CoV-2 .
9-β-D-Arabinofuranosylguanine is a Guanosine (HY-N0097) analog and shows highaffinity for deoxyguanosine kinase (dGK) with a Km of 8.0 μM. 9-β-D-Arabinofuranosylguanine can be used for the research of T-cell lymphoblastic disease .
Polymyxin B is an antibiotic. Polymyxin B inhibits Gram-negative infections by binding to the LPS of the bacterial wall with highaffinity. Polymyxin B neutralizes the effect of endotoxin. Polymyxin B induces bacterial death by increasing its permeability. Polymyxin B is used in endotoxemia research .
Propionyl-L-carnitine is a carnitine derivative and has a highaffinity for muscular carnitine transferase. Propionyl-L-carnitine increases cellular carnitine content, thereby allowing free fatty acid transport into the mitochondria. Propionyl-L-carnitine alleviates the symptoms of PAD through a metabolic pathway, thereby improving exercise performance .
RS-127445 hydrochloride is a selective, highaffinity, orally bioavailable 5-HT2B receptor antagonist with a pKi of 9.5. RS-127445 hydrochloride shows 1000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites .
Ro 41-1049 hydrochloride is a reversible and selective inhibitor of monoamine oxidase-A (MAO-A). An homogeneous population of highaffinity binding sites for [ 3H]Ro 41-1049 is found in membrane preparations from human frontal cortex and placenta (Kd values of 16.5 and 64.4 nM, respectively) .
Pioglitazone-d4 is a deuterium labeled Pioglitazone. Pioglitazone (U 72107) is a potent and selective PPARγ agonist with highaffinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 and 0.99 μM for human and mouse PPARγ, respectively[1].
SR10067 is a potent, selective and brain penetrant REV-ERB agonist. SR10067 has highaffinity for Rev-Erbβ and Rev-Erbα with IC50 values of 160 nM and 170 nM, respectively. SR10067 can be used for the research of metabolic diseases and neuropsychiatric disorders .
N-Methylcytisine (Caulophylline), a tricyclic quinolizidine alkaloid, exerts hypoglycaemic, analgesic and anti-inflammatory activities. N-methylcytisine is a selective ligand of nicotinic receptors of acetylcholine in the central nervous system and has a highaffinity (Kd = 50 nM) to nicotinic acetylcholine receptors (nAChR) from squid optical ganglia .
Imetit dihydrobromide (VUF 8325 dihydrobromide) is a highaffinity and potent agonist of histamine H3 and H4 receptors, with Ki values of 0.3 and 2.7 nM, respectively. Imetit mimics histamine effect in triggering a shape change in eosinophils (EC50=25 nM) .
RS-127445 is a selective, highaffinity, orally bioavailable 5-HT2B receptor antagonist with a pKi of 9.5. RS-127445 shows 1000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites .
Nelonicline (ABT-126) citrate is an orally active and selective α7 nicotinic receptor agonist with highaffinity to α7 nAChRs in human brain (Ki=12.3 nM). Nelonicline citrate is used for the research of shizophrenia and Alzheimer's disease .
Sabatolimab (MBG453) is a high-affinity, humanized, IgG4 (S228P) antibody targeting TIM-3, an inhibitory receptor that regulates adaptive and innate immune responses. Sabatolimab is a potential immunosuppression agent that can target TIM-3 on immune and myeloid cells .
Lerisetron is a potent 5-HT3 antagonists and possess high-affinity binding for the 5-HT3 receptors with pKi value of 9.2. Lerisetron has a potent ability to inhibit the 5-HT-evoked reflex bradycardia in urethane-anesthetized rats .
Imsidolimab (ANB 019) is a high-affinity, humanized monoclonal antibody of anti-IL-36R. Imsidolimab antagonizes IL-36 cytokine signal transduction. Imsidolimab has potential application in generalized pustular psoriasis (GPP) and other inflammatory skin diseases .
PGN-9856 is a selective and highaffinity (pKi ≥ 8.3) ligand at EP2 receptor. PGN-9856 is a potetn and non-prostanoid EP2 receptor agonist (pEC50 ≥ 8.5). PGN-9856 shows anti-inflammatory and anti-glaucoma activities .
TMPA is a high-affinityNur77 antagonist that binds to Nur77 leading to the release and shuttling of LKB1 in the cytoplasm to activate AMPKα. TMPA effectively lowers blood glucose and attenuates insulin resistance in type II db/db, high-fat diet and streptozotocin-induced diabetic mice. TMPA reduces RICD (restimulation-induced cell death) in human T cells, can also be used in studies of cancer and T-cell apoptosis dysregulation .
AT2R antagonist 1 (compound 21) is a potent and high selective AT2R (angiotensin II AT2 receptor) ligand. AT2R antagonist 1 exhibits a fair AT2Raffinity, with a Ki of 29 nM. AT2R antagonist 1 also inhibits common agent-metabolizing CYP enzymes. AT2R antagonist 1 shows high stability in human, rat and mouse liver microsomes .
Kurtoxin is a selective Cav3 (T-type) voltage-gated Ca 2+ channel gating inhibitor with a Kd of 15 nM for Cav3.1 (α1G T-type) Ca 2+ channel. Kurtoxin can interact with highaffinity with native neuronal high-threshold L-type, N-type, and P-type Ca 2+ channels in central and peripheral neurons. Kurtoxin also shows cross-reactivity with voltage-gated Na + channel .
human GALP (3-32) (Galanin-like peptide (3-32)) is a potent galanin receptor agonist with highaffinity for both GalR1 (IC50=33 nM) and GalR2 (IC50=15 nM) in a competitive binding study. human GALP (3-32) exhibits the high potency in altering the extracellular acidification rate of SH-SY5Y cells transfected with GalR2 (EC50=360 nM) .
OTS964 hydrochloride is an orally active, highaffinity and selective TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor with an IC50 of 28 nM . OTS964 hydrochloride is also a potent inhibitor of the cyclin-dependent kinase CDK11, which binds to CDK11B with a Kd of 40 nM .
LY2940094 (BTRX-246040) is a potent, selective and orally available nociceptin receptor (NOP receptor) antagonist with highaffinity (Ki=0.105 nM) and antagonist potency (Kb=0.166 nM). LY2940094 reduces ethanol self-administration in animal models .
Galanin Receptor Ligand M35 TFA is a high-affinity ligand and antagonist of galanin receptor (Kd=0.1 nM). Galanin Receptor Ligand M35 TFA exerts a Ki values of 0.11 and 2.0 nM for human galanin receptor type 1 and 2, respectively .
F1324 TFA is a potent, highaffinity peptidic inhibitor of B cell lymphoma 6 (BCL6), with an IC50 of 1 nM. F1324 TFA exhibits binding t1/2 value of 441 s and has strong inhibition activity against BCL6 PPI .
AZD1940 is an orally active, highaffinitycannabinoid CB1/CB2 receptor agonist with pKi values of 7.93 and 9.06 for human CB1R and CB2R, respectively. AZD1940 shows a robust analgesia action .
Trospium-d8 (chloride) is the deuterium labeled Trospium chloride. Trospium chloride is an orally active, specific and competitive antagonist of muscarinic cholinergic receptors (mAChRs), with antimuscarinic activity. Trospium chloride binds to muscarinic receptors M1, M2 and M3 with highaffinity, but not nicotinic, cholinergic receptors[1][2].
SOR-C13, a carboxy-terminal truncated peptide, is a high-affinityTRPV6 antagonist with an IC50 value of 14 nM. TRPV6 is a non-voltage gated calcium channel that is associated with malignancy and poor prognosis in breast cancer. SOR-C13 has anticancer activity .
Tuvirumab (OST 577; SDZ-OST 577) is a human IgG1 subclass monoclonal antibody directed against HBV surface antigen (HBsAg). Tuvirumab binds specifically and with highaffinity (K=3.6 nM) to HBsAg. Tuvirumab has the potential for chronic hepatitis B research .
PAOPA, an analog of L-proline-l-leucine-glycine amide (PLG) peptide, is an allosteric modulator of Dopamine D2 Receptor. PAOPA can effectively reduce behavioral abnormalities in rodent models of schizophrenia. PAOPA increases the highaffinity dopamine D2 receptor and promotes its binding to agonists .
LY255582 is a pan-opioid antagonist and has highaffinity for mu, delta, and kappa receptors (Ki: 0.4 nM, 5.2, 2.0 nM respectively). LY255582 can decrease food intake and body weight. LY255582 can be used for the research of obesity .
Phox-I2 is a selective inhibitor of p67 phox-Rac1 interaction, binds to p67 phox with highaffinity with a Kd of ~150 nM. Phox-I2 is a NADPH oxidase 2 (NOX2) inhibitor and inhibits reactive oxygen species (ROS) production .
AM841 is a high-affinity electrophilic ligand. AM841 interacts covalently with a cysteine in helix six and activates the CB1 cannabinoid receptor. AM841 reduces Forskolin (HY-15371)-stimulated cAMP accumulation. AM841 also slows gastrointestinal motility .
YG1702 is a potent ALDH18A1-specific inhibitor. YG1702 attenuates the growth of MYCN-amplified NB and down-regulates MYCN. YG1702 physically interacts with ALDH18A1 with a highaffinity and might potentially affect its enzymatic activity .
UCSF924 is a potent and specific dopamine D4 receptor (DRD4) partial agonist with a EC50 of 4.2 nM. UCSF924 has a high-affinity with a Ki value of 3 nM for DRD4 and shows no measurable affinity for D2, D3 or the F261V/L328F D4 mutant. UCSF924 is a 7.4-fold bias toward arrestin over Gαi/o signaling, referenced to quinpirole .
Roxindole hydrochloride (EMD 38362), an indot-alkyl-pipenidine, is a potent agonist at dopamine autoreceptors, with an affinity for the D2-like subtype in the low nanomolar range. Roxindole can be used for the research of positive and negative schizophrenic symptoms. Roxindole is a 5-HT1A agonist and 5-HT uptake inhibitor with highaffinity for 5-HT1A (IC50=0.9 nM). Antipsychotic and antidepressant activities .
Levobetaxolol is a potent and highaffinityβ-adrenergic antagonist with IC50 values of 33.2, 2970, 709 nM for guinea pig atrial β1, tracheal β2 and rat colonic β3 receptors, respectively. Levobetaxolol reduces IOP (intraocular pressure). Levobetaxolol exhibits a micromolar affinity for L-type Ca21-channels. Levobetaxolol decreases the effects of ischaemia/reperfusion injury in rats. Levobetaxolol has the potential for the research of glaucoma .
(Rac)-WAY-161503 hydrochloride is a potent, selective, highaffinity5-HT2C receptor agonist with a Ki of 4 nM and an EC50 of 12 nM. (Rac)-WAY-161503 hydrochloride displays higher affinity for 5-HT2C than 5-HT2A and 5-HT2B receptors. (Rac)-WAY-161503 hydrochloride has anti-obesity and antidepressant effects .
Seltorexant hydrochloride (JNJ-42847922 hydrochloride) is an orally active, high-affinity, and selective OX2R antagonist (pKi values of 8.0 and 8.1 for human and rat OX2R). Seltorexant hydrochloride crosses the blood-brain barrier and quickly occupies OX2R binding sites in the rat brain .
BA 1 is a potent agonist for the bombesin (BB) family of receptors. BA 1 binds with highaffinity to Bombesin receptor subtype-3 (BRS3), gastrin releasing peptide receptor (GRPR), neuromedin B receptor (NMBR) with IC50s of 6, 0.4, 2.5 nM .
Biotinylated-JQ1 (Biotin-JQ1) is a biotinylated derivative of JQ1 with highaffinity for the bromodomain of BRD4. Biotinylated-JQ1 inhibits MM1.S multiple myeloma cells proliferation with the EC50 of 0.4 μM .
OS-3-106 is a potent, BBB-penetrated and selective dopamine D3 receptor (D3R) agonist. OS-3-106 binds with highaffinity (Ki = 0.2 nM) at the D3R. OS-3-106 can be used for psychoactivator addiction research .
THK-523 has demonstrated its highaffinity and selectivity for tau pathology both in vitro and in vivo. 18F-THK523 is a potent tau imaging radiotracer. 18F-THK523 is a potent in vivo tau imaging ligand for Alzheimer's disease .
Emapalumab (NI-0501) is a human monoclonal IgG1 antibody that noncompetitively inhibits IFN-γ. Emapalumab binds with highaffinity (Kd= 1.4 pM) to both free IFN-γ as well as IFN-γ bound to its receptor. Emapalumab can be used in research of hemophagocytic lymphohistiocytosis (HLH) .
(Tyr0)-Urocortin, rat is a high-affinity agonist of corticotropin-releasing factor receptor type 1 (CRF-R1) and type 2 (CRF-R2). (Tyr0)-Urocortin, rat shows inhibitory binding constants (Ki) of 1-2 nM .
HIV-IN-9 (Compound 2b) is a HIV inhibitor (IC50: 6.65 μg/mL), and has high binding affinity with HIV-RT. HIV-IN-9 also inhibits CYP3A4, CYP1A2, CYP2C1, and CYP2D6 .
APT STAT3 is a specific STAT3-binding peptide. APT STAT3 can bind STAT3 with high specificity and affinity (~231 nmol/L). APT STAT3 is a tractable agent for translation to target the broad array of cancers harboring constitutively activated STAT3 .
Anticancer agent 183 (example 48) is a non-agonistic PPARG modulator. Anticancer agent 183 has a highaffinity to PPARG (PPARγ). Anticancer agent 183 inhibits kinase-mediated phosphorylation of PPARG. Anticancer agent 183 can used for research on metabolic diseases to avoid side effects .
α-Zearalenol (Standard) is the analytical standard of α-Zearalenol. This product is intended for research and analytical applications. α-Zearalenol is a Mycotoxin with highaffinity for the estrogen receptors (ER), α-Zearalenol is the derivative of zearalenone (ZEN), causes reproductive disorders in animals, due to its xenoestrogenic effects .
RU 59063 is an N-substituted arylthiohydantoin compound with antiandrogenic activity and high relative binding affinity for the rat androgen receptor. RU 59063 is a nonsteroidal androgen receptor that functions as a radioactive AR radioprobe (Ki: 0.71 nM, rAR) when its trifluoromethyl group is replaced by a similar hydrophobic iodine atom .
Deramciclane has a highaffinity for 5-HT2A and 5-HT2C receptors; it acts as an antagonist at both receptor subtypes and has inverse agonist properties at the 5-HT2C receptors without direct stimulatory agonist.
Mizolastine is an orally active, highaffinity and specific peripheral histamine H1 receptor antagonist (second generation antihistamine). Mizolastine effectively inhibits mRNA expression of VEGF165, VEGF120, TNF-α and KC. Mizolastine can be used in studies of allergic rhinitis and chronic idiopathic urticarial .
Mizolastine dihydrochloride is an orally active, highaffinity and specific peripheral histamine H1 receptor antagonist (second generation antihistamine). Mizolastine dihydrochloride effectively inhibits mRNA expression of VEGF165, VEGF120, TNF-α and KC. Mizolastine dihydrochloride can be used in studies of allergic rhinitis and chronic idiopathic urticarial .
Mavatrep (JNJ-39439335) is an orally active, selective and potent TRPV1 antagonist with highaffinity for hTRPV1 channels (Ki=6.5 nM). Mavatrep antagonizes capsaicin-induced Ca 2+ influx with an IC50 value of 4.6 nM. Mavatrep can be used in some studies of neuropathic pain .
L-371,257 is an orally bioavailable, non-blood-brain barrier penetrant, selective and competitive antagonist of oxytocin receptor (pA2=8.4) with highaffinity at both the oxytocin receptor (Ki=19 nM) and vasopressin V1a receptor (Ki=3.7 nM) .
PCSK9 degrader 1 (Compound 16) is a small molecule ligand for proprotein convertase substilisin-like/kexin type 9 (PCSK9) and shows highaffinity to PCSK9 with a Ki of 107 nM. PCSK9 degrader 1 can involve in a protein-protein interaction with the low-density lipoprotein (LDL) receptor .
2',3'-cGAMP sodium (2'-3'-cyclic GMP-AMP sodium) is a endogenous cGAMP in mammalian cells. 2',3'-cGAMP sodium binds to STING with a highaffinity and is a potent inducer of interferon-β (IFNβ). 2',3'-cGAMP sodium is produced in mammalian cells in response to DNA in the cytoplasm .
cis-Urocanic acid is a 5-HT2A receptor agonist. cis-Urocanic acid binds to 5-HT receptor with relatively highaffinity (Kd=4.6 nM). cis-Urocanic acid is an immune modulator that induces immunosuppression by binding to the 5-HT2A receptor .
BA 1 TFA is a potent agonist for the bombesin (BB) family of receptors. BA1 binds with highaffinity to Bombesin receptor subtype-3 (BRS3), gastrin releasing peptide receptor (GRPR), neuromedin B receptor (NMBR) with IC50s of 6, 0.4, 2.5 nM .
GaTx2 is a seletive and a highaffinity inhibitor of ClC-2 channels with a voltage-dependent apparent KD of ∼20 pM. GaTx2 is a peptide toxin inhibitor from Leiurus quinquestriatus hebraeus venom. GaTx2 is useful in determining the role and the membrane localization of ClC-2 in specific cell types .
(R)-Propranolol hydrochloride is a less active enantiomer of the β-adrenoceptor antagonist propranolol (HY-B0573). Propranolol is a nonselective β-adrenergic receptor (βAR) antagonist, has highaffinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively .
2',3'-cGAMP (2'-3'-cyclic GMP-AMP) is a endogenous cGAMP in mammalian cells. 2',3'-cGAMP binds to STING with a highaffinity and is a potent inducer of interferon-β (IFNβ). 2',3'-cGAMP is produced in mammalian cells in response to DNA in the cytoplasm .
VU0424465 is a potent and partial PAM (positive allosteric modulator)-agonist for mGlu5 mediated iCa 2+ mobilization. VU0424465 exhibits highaffinity at MPEP allosteric binding site, with a Ki value of 11.8 nM. VU0424465 is also a agonist for pERK1/2 in cortical neurons .
Clazakizumab is a monoclonal antibody with highaffinity and specificity for the IL-6 (interleukin-6) cytokine. Clazakizumab may be helpful in inhibiting the cytokine response to SARS-CoV-2 in COVID-19. Clazakizumab can be used for the research of psoriatic arthritis (PsA) and renal antibody-mediated rejection .
5,5'-Dinitro BAPTA AM is a membrane-permeant, high-affinitycalcium chelator, it can be used for investigation of the role of cytosolic Ca 2+. 5,5'-Dinitro BAPTA AM can be loaded by incubation into live cells, and is cleaved by cytosolic esterases to liberate the active tetra-carboxylate ligand .
Abrezekimab (VR 942) contains CDP7766, a humanized, high-affinity, neutralizing, anti-human-IL-13 antibody fragment that binds to IL-13. Abrezekimab prevents binding to the IL-13Rα1 subunit. Abrezekimab can be used in research of asthma .
SOR-C13 TFA, a carboxy-terminal truncated peptide, is a high-affinityTRPV6 antagonist with an IC50 value of 14 nM. TRPV6 is a non-voltage gated calcium channel that is associated with malignancy and poor prognosis in breast cancer. SOR-C13 TFA has anticancer activity .
Latozinemab (AL001) is a recombinant human anti-Sortilin monoclonal antibody. Latozinemab effectively binds Sortilin with a highaffinity and blocks the interaction between progranulin protein (PGRN) and Sortilin receptor. Latozinemab has the potential for progranulin gene (GRN) mutations causative of Frontotemporal dementia (FTD) (FTD-GRN) research .
KSK94 is a high-affinityhistamine H3 receptor antagonist, with Kis of 7.9, 2958, 75.2 nM for H3 receptor, sigma-1, sigma-2 receptor respectively. KSK94 can be used for research of nociceptive and neuropathic pain .
5,6-trans-Travoprost is the isomer of Travoprost (HY-B0584), and can be used as an experimental control. Travoprost (Fluprostenol isopropyl ester), an isopropyl ester proagent, is a highaffinity, selective FP prostaglandin full receptor agonist. Travoprost has the ocular hypotensive efficacy and has the potential for glaucoma and ocular hypertension .
(R)-L 888607 is the isomer of L 888607 (HY-111271), and can be used as an experimental control. L 888607 is a potent, selective, stable and orally active CRTH2 agonist. L 888607 has highaffinity for the human CRTH2 receptor with a Ki value of 4 nM. L 888607 can be used for the research of several physiological events and metabolite .
TAOA AM Ester trimethyl lock is a high-affinity fluorescent prodrug-like inhibitor of the excitatory amino acid transporter (EAAT). It can penetrate the cell membrane and be activated by hydrolysis by endogenous cell esterases to form active EAAT inhibitors. TAOA AM Ester trimethyl lock can be used to study neurodegeneration and neuronal cell death .
10,12-Tricosadiynoic acid is a highly specific, selective, highaffinity and orally active acyl-CoA oxidase-1 (ACOX1) inhibitor. 10,12-Tricosadiynoic acid can treat high fat diet- or obesity-induced metabolic diseases by improving mitochondrial lipid and ROS metabolism . 10,12-Tricosadiynoic acid is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Pioglitazone (U 72107) is an orally active and selective PPARγ (peroxisome proliferator-activated receptor) agonist with highaffinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 and 0.99 μM for human and mouse PPARγ, respectively. Pioglitazone can be used in diabetes research .
L-701324 is a potent, orally active NMDA receptor antagonist that antagonizes the activity of the NMDA receptor by blocking its glycine B binding site. L-701324 binds with highaffinity to rat brain membranes (IC50=2 nM). L-701324 has antidepressant activity .
TCS-OX2-29 is a potent, highaffinities and selective orexin-2 receptor (OX2R) antagonist with an IC50 value of 40 nM and a pKI value of 7.5. TCS-OX2-29 displays ~250-fold selectivity for OX2 over OX1 .
LAH4, an alpha-helix of the designed amphipathic peptide antibiotic, exhibits potent antimicrobial, nucleic acid transfection and cell penetration activities. LAH4 possesses high plasmid DNA delivery capacities. LAH4 has a strong affinity for anionic lipids found in the outer membrane of bacterial membranes .
Roluperidone (CYR-101) is a novel cyclic amide derivative that has high equipotent affinities for 5-HT2A and sigma-2 receptors (Ki of 7.53 nM and 8.19 nM for 5-HT2A and sigma-2, respectively).
5-HT3 antagonist 3 (Compound 15b) is a high-affinity5-HT3 receptor antagonist. 5-HT3 antagonist 3 binds to 5-HT3 receptors in rat brain cortical membranes with Ki of 0.25 nM .
SP4206 is an IL-2/IL-2Rα interaction inhibitor. SP4206 binds with highaffinity (Kd=70 nM) to IL-2 and blocks binding to its natural receptor IL-2Rα (Kd=10 nM) .
Iptacopan (LNP023) is a first-in-class, orally bioavailable, highly potent and highly selective factor B inhibitor with an IC50 value of 10 nM. Iptacopan shows direct, reversible, and high-affinity binding to human factor B with a KD of 7.9 nM. Iptacopan targets the underlying cause of complement 3 glomerulopathy (C3G) .
Barnidipine hydrochloride (Mepirodipine hydrochloride) is an L-type calcium antagonist (CaA) with highaffinity for [ 3H] initrendipine binding sites (Ki=0.21 nmol/l), has selective action against CaA receptors . Barnidipine hydrochloride (Mepirodipine hydrochloride) is an antihypertensive agent and acts by the reduction of peripheral vascular resistance secondary to its vasodilatory action .
Barnidipine (Mepirodipine) is an L-type calcium antagonist (CaA) with highaffinity for [ 3H] initrendipine binding sites (Ki=0.21 nmol/l), has selective action against CaA receptors . Barnidipine (Mepirodipine) is an antihypertensive agent and acts by the reduction of peripheral vascular resistance secondary to its vasodilatory action .
AZ10606120 dihydrochloride is a selective, highaffinity antagonist for P2X7 receptor (P2X7R) at human and rat with an IC50 of about 10 nM. AZ10606120 dihydrochloride is little or no effect at other P2XR subtypes. AZ10606120 dihydrochloride has anti-depressant effects and reduces tumour growth .
NDI-091143 is a potent and high-affinityhuman ATP-citrate lyase (ACLY) inhibitor with an IC50 of 2.1 nM (ADP-Glo assay), a Ki of 7.0 nM and a Kd of 2.2 nM. NDI-091143 inhibits ACLY catalysis allosterically, by stabilizing large conformational changes in the citrate domain that indirectly block the binding and recognition of citrate .
Anti-MERS-3A1 mAb (MERS-3A1) is a human monoclonal IgG1 antibody with the high binding affinity produced in CHO cells.
Anti-MERS-3A1 mAb bocks the binding of MERS-CoV spike protein to DPP4 receptor .
DG-041 is a potent, highaffinity and selective EP3 receptor antagonist with IC50s of 4.6 nM and 8.1 nM in the binding and FLIPR assay, respectively. DG-041 inhibits PGE2 facilitation of platelet aggregation. DG-041 crosses the blood-brain barrier .
K-(D-1-Nal)-FwLL-NH2 is a highaffinity, potent and inverse ghrelin receptor agonist (EC50=3.4 nM, Ki=4.9 nM). K-(D-1-Nal)-FwLL-NH2 can be used for the research of obesity .
Hemicholinium 3 is a competitive inhibitor of the highaffinity choline transporter (HACU) with a Ki value of 25 nM. Hemicholinium 3, a neuromuscular blocking agent which inhibits the synthesis and the release of acetylcholine (ACh) . Hemicholinium 3 inhibits the Epibatidine-evoked contraction and [ 3H]acetylcholine release with IC50s of 897 nM and 693 nM, respectively .
TCS-OX2-29 (hydrochloride) is a potent, highaffinities and selective orexin-2 receptor (OX2R) antagonist with an IC50 value of 40 nM and a pKI value of 7.5. TCS-OX2-29 displays ~250-fold selectivity for OX2 over OX1 .
SNX-0723 is a potent Hsp90 Inhibitor with anti-Plasmodium activity. SNX-0723 shows high binding affinity for HsHsp90 and PfHsp90 with Kis of 4.4 and 47 nM, respectively. SNX-0723 inhibits liver-stage P. berghei ANKA parasites with the EC50 of 3.3 μM .
Pioglitazone (U 72107) potassium is an orally active and selective PPARγ (peroxisome proliferator-activated receptor) agonist with highaffinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 μM and 0.99 μM for human and mouse PPARγ, respectively. Pioglitazone potassium can be used in diabetes research .
HA-IN-1 (compound 5g) is a Hemagglutinin (HA) ligand with highaffinity, targeting to the trypsin cleavage site of HA. HA-IN-1 inhibits HA-mediated membrane fusion and reduces the pulmonary virus titer in vivo. HA-IN-1 is a potential influenza A virus (IAV) inhibitor, and an anti-influenza agent .
Biphalin TFA, a BBB-penetrable opioid peptide analog, contains two active enkephalin pharmacophores. Biphalin TFA has highaffinity for opioid receptors. Biphalin TFA shows analgesic effect in acute, neuropathic, and chronic animal pain models. Biphalin TFA is also an antiviral, antiproliferative, anti-inflammatory, and neuroprotective agent .
SW1 aptamer sodium is a high-affinity DNA aptamer (Kd: 123.62 nM) that targets liver cancer SMMC-7721 cells and targets intracellular components within the nucleus. SW1 aptamer sodium can also identify various other types of cancer cells and tissues, serving as an effective molecular probe for clinical cancer diagnosis .
CGP 12177 ((±)-CGP 12177) hydrochloride is a β Adrenergic Receptor Ligand. CGP 12177 hydrochloride is a highaffinity antagonist of β1- and β2-AR. CGP 12177 hydrochloride is also shown to interact, with a lower affinity, with the β3-AR and to exhibit a partial agonist activity on rodent and human β3-AR. CGP 12177 hydrochloride exhibits partial agonist properties for α1-AR in rat pulmonary artery .
Prolactin Releasing Peptide (1-31), human is a highaffinityGPR10 ligand that cause the release of the prolactin. Prolactin Releasing Peptide (1-31) binds to GPR10 for human and rats with Ki values of 1.03 nM and 0.33 nM, respectively. Prolactin Releasing Peptide (1-31) can be used for the research of the hypothalamo-pituitary axis .
ZT-12-037-01 is a STK19-targeted inhibitor, has a high-affinity interaction with STK19 protein and inhibits oncogenic NRAS-driven melanocyte malignant transformation. ZT-12-037-01 is an ATP-competitive inhibitor, inhibiting phosphorylation of NRAS (major isoform of Ras family) with an IC50 of 24 nM .
JNJ-47965567 is a centrally permeable, high-affinity, selective P2X7 antagonist, with pKis of 7.9 and 8.7 for human and rat P2X7, respectively. JNJ-47965567 can be used to probe the role of central P2X7 in rodent models of CNS pathophysiology .
Sialyl-Lewis X (sLeX) is a sialylated fucosylated tetrasaccharide, an endogenous antigen. Sialyl-Lewis X is a high-affinityligand for selectins (E-, P-, and L-selectin) . Sialyl-Lewis X binds to ELAM-1 and CD62 and has the ability to inhibits CD62-mediated neutrophil recruitment to sites of inflammation .
R-BC154 acetate is a selective fluorescent α9β1 integrin antagonist. R-BC154 acetate acts as a useful highaffinity, activation dependent integrin probe, which can be used to investigate α9β1 and α4β1 integrin binding activity .
ELA-11(human) TFA is a highaffinity apelin receptor agonist (Ki=14 nM). ELA-11(human) TFA is a bioactive fragment of ELA-32. ELA-11(human) TFA inhibits forskolin-induced cAMP production and stimulates β-arrestin recruitment in vitro.
TPP-1 is a potent inhibitor of the PD-1/PD-L1 interaction. TPP-1 binds specifically to PD-L1 with a highaffinity (KD=95 nM). TPP-1 inhibits human tumor growth in vivo via reactivating T-cell function .
LAH4 TFA, an alpha-helix of the designed amphipathic peptide antibiotic, exhibits potent antimicrobial, nucleic acid transfection and cell penetration activities. LAH4 TFA possesses high plasmid DNA delivery capacities. LAH4 TFA has a strong affinity for anionic lipids found in the outer membrane of bacterial membranes .
Cabergoline-d6 is deuterium labeled Cabergoline. Cabergoline is an ergot derived-dopamine D2-like receptor agonist that has highaffinity for D2, D3, and 5-HT2B receptors (Ki=0.7, 1.5, and 1.2, respectively).
MRK-623 (Compound 14k) is an orally active, high-affinityGABAA receptor agonist, with the Ki values of 0.85 nM, 3.7 nM, 4.0 nM, and 0.53 nM for α1, α2, α3, and α5, respectively. MRK-623 shows anxiolytic effect .
STAT6-IN-1 (compound 19a) is a STAT6 inhibitor with a highaffinity for the SH2 domain of STAT6 (IC50=0.028 µM). STAT6-IN-1 can be used in studies of allergic lung disease, allergic rhinitis, chronic obstructive pulmonary disease or cancer .
Prolactin Releasing Peptide (1-31), human (acetate) is a highaffinityGPR10 ligand that causes the release of the prolactin. Prolactin Releasing Peptide (1-31) binds to GPR10 for human and rats with Ki values of 1.03 nM and 0.33 nM, respectively. Prolactin Releasing Peptide (1-31) can be used for the research of the hypothalamo-pituitary axis .
Deoxyneocryptotanshinone, a natural tanshinone, is a highaffinityBACE1 (Beta-secretase) inhibitor with an IC50 value of 11.53 μM. Deoxyneocryptotanshinone shows a promising dose-dependent inhibition of protein tyrosine phosphatase 1B (PTP1B) with an IC50 value of 133.5 μM. Deoxyneocryptotanshinone can be used for Alzheimer's disease research .
Dostarlimab (TSR-042) is a humanized anti-PD-1 monoclonal antibody. Dostarlimab binds with highaffinity to human PD-1 and competitively inhibits its interaction with its ligands, PD-L1 and PD-L2, with IC50s of 1.8 and 1.5 nM, respectively .
A1/A3 AR antagonist 3 is an A1R/A3R dual antagonist with highaffinity at low-micromolar to low-nanomolar. A1/A3 AR antagonist 3 can be used for the research of chronic heart diseases .
HMG-CoA Reductase-IN-1 is a HMG-CoA reductase inhibitor. HMG-CoA Reductase-IN-1has highHMGR inhibitory activity and OATP1B1affinity with pIC50 and pKm values of 8.54 and 1.98, respectively. HMG-CoA Reductase-IN-1 can be used for the research of hypercholesterolemia .
SARS-CoV-2-IN-57 (compound (+)-R-26) is a potent inhibitor of SARS-CoV-2 (IC50: 80 nM). SARS-CoV-2-IN-57 has highaffinity for Sigma Receptor with Kis of 13.6 nM (S1R) and 14.4 nM (S2R) respectively .
(Pro3) GIP, human TFA is an efficacious, stable and specific human GIP receptor (hGIPR) full agonist. (Pro3) GIP, human TFA has high binding affinity for human GIPR with Ki/ Kd value of 0.90 nM. (Pro3) GIP, human TFA human can be used for the research of obesity-related diabetes .
TSLP binder-1 (compound 46) is a bicyclic peptide, which binds to thymic stromal lymphopoietin (TSLP) at the site used by IL-7Rα subunit, shows highaffinity for TSLP, with KD of 13 nM. TSLP binder-1 reveals good stability in rat plasma and rat lung S9 fraction .
(6S)-Tetrahydrofolic acid is 1000-fold more active than the (6R) form at promoting the binding of fluorodeoxyuridylate to thymidylate synthase and 600-fold more active as a growth factor of P. cerevisiae. (6S)-Tetrahydrofolic acid also has a low affinity and high dissociation rate for folate-binding protein .
Xaliproden hydrochloride (SR57746A) is a potent, selective and orally active agonist of 5-HT1A receptor, shows a highaffinity for 5-HT1A specific binding sites in the rat hippocampus (IC50=3 nM). Xaliproden hydrochloride is also a selective antagonist of dopamine D2 receptor, has moderate affinity (IC50=0.1-1 μM). Xaliproden hydrochloride exhibits anti-depression and anti-anxiety effects, and it may possess therapeutic potential for the research of neurodegenerative diseases .
Nebivolol (R 065824) is an orally active beta receptor blocker and has the high beta(1)-receptor affinity. Nebivolol has direct vasodilator properties and adrenergic blocking characteristics. Nebivolol can be used for the research of kinds of diseases such as hypertension, coronary artery disease, congestive heart failure and ischemic heart disease .
Nebivolol (R 065824) hydrochloride is an orally active beta receptor blocker and has the high beta(1)-receptor affinity.Nebivolol hydrochloride has direct vasodilator properties and adrenergic blocking characteristics. Nebivolol hydrochloride can be used for the research of kinds of diseases such as hypertension, coronary artery disease, congestive heart failure and ischemic heart disease .
UMI-77 is a selective Mcl-1 inhibitor, which shows high binding affinity to Mcl-1 (IC50=0.31 μM). UMI-77 binds to the BH3 binding groove of Mcl-1 with Ki of 490 nM, showing selectivity over other members of anti-apoptotic Bcl-2 members.
Batefenterol (GSK961081;TD-5959) is a novel muscarinic receptor antagonist and β2-adrenoceptor agonist; displays highaffinity for hM2, hM3 muscarinic and hβ2-adrenoceptor with Ki values of 1.4, 1.3 and 3.7 nM, respectively.
MA242 is a specific dual inhibitor of MDM2 and NFAT1. MA242 directly binds both MDM2 and NFAT1 with highaffinity, induces their protein degradation, and inhibits NFAT1-mediated transcription of MDM2. MA242 induces apoptosis in pancreatic cancer cell lines regardless of p53 status .
Cabergoline-d5 is the deuterium labeled Cabergoline. Cabergoline is an ergot derived-dopamine D2-like receptor agonist that has highaffinity for D2, D3, and 5-HT2B receptors (Ki=0.7, 1.5, and 1.2, respectively)[1][2].
Pioglitazone-d4 (alkyl) (U 72107-d4 (alkyl)) is the deuterium labeled Pioglitazone. Pioglitazone (U 72107) is a potent and selective PPARγ agonist with highaffinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 and 0.99 μM for human and mouse PPARγ, respectively[1][2].
Seltorexant (JNJ-42847922) is an orally active, high-affinity, and selective orexin-2 receptor (OX2R) antagonist (pKi values of 8.0 and 8.1 for human and rat OX2R). Seltorexant (JNJ-42847922) crosses the blood-brain barrier and quickly occupies OX2R binding sites in the rat brain .
BIIL-260 hydrochloride is a potent and long-acting orally active leukotriene B(4) receptor LTB4 antagonist, with anti-inflammatory activity. BIIL-260 hydrochloride interacts with the LTB4 receptor in a saturable, reversible, and competitive manner, has highaffinity to the LTB4 receptor on isolated human neutrophil cell membranes with Ki values of 1.7 nM .
KGA-2727 is a first selective, high-affinity and orally active SGLT1 inhibitor with Kis of 97.4 nM and 43.5 nM for human and rat SGLT1, respectively. The selectivity ratios (Ki for SGLT2/Ki for SGLT1) of KGA-2727 are 140 (human) and 390 (rat). KGA-2727 has antidiabetic efficacy .
Facinicline hydrochloride (RG3487 hydrochloride) is an orally active nicotinic α7 receptor partial agonist, with a Ki of 6 nM for α7 human nAChR. Facinicline hydrochloride (RG3487 hydrochloride) improves cognition and sensorimotor gating in rodents. Facinicline hydrochloride (RG3487 hydrochloride) shows highaffinity (antagonist) to 5-HT3Rs with a Ki value of 1.2 nM .
Levocabastine (R 50547) hydrochloride is a potent and selective histamine H1-receptor antagonist. Levocabastine hydrochloride is also a selective, highaffinityneurotensin receptor subtype 2 (NTR2) antagonist, with a Ki of 17 nM for mNTR2. Levocabastine hydrochloride can act as a VLA-4 antagonist, interferes with conjunctival eosinophil infiltration in allergic conjunctivitis (AC) .
LY2940094 (BTRX-246040) tartrate is a potent, brain penetrant, selective and orally available N/OFQ peptide (NOP) receptor antagonist with highaffinity (Ki=0.105 nM) and antagonist potency (Kb=0.166 nM). LY2940094 tartrate reduces Ethanol self-administration and Ethanol seeking in animal models .
Emedastine- 13C,d3 (fumarate) is the 13C- and deuterium labeled Emedastine. Emedastine is an orally active, selective and highaffinity histamine H1 receptor antagonist with a Ki value of 1.3 nM. Emedastine is a benzimidazole derivative with potent antiallergic properties and used for allergic rhinitis, allergic skin diseases and allergic conjunctivitis[1][2][3].
Anti-MRSA agent 3 (compound 18) has highly inhibitory activity against Methicillin-resistant Staphylococcus aureus (MRSA) with MIC of 0.098 μg/ml, and low cytotoxicity in normal cells. Anti-MRSA agent 3 has relatively strong ability to destroy bacterial cell wall and membrane, high binding affinity to bacterial genomic DNA .
Tislelizumab, a monoclonal antibody with high binding affinity to the PD-1 receptor, minimizes Fcγ receptor binding on macrophages, thereby abrogating antibody-dependent phagocytosis, a mechanism of T cell clearance and potential resistance to anti-PD-1 research. Tislelizumab can be used for the research of advanced squamous non-small-cell lung cancer .
GnRH-R antagonist 1 (compound 21a) is an orally safe and membrane-permeable GnRH-R antagonist with high binding affinity (IC50=0.57 nM) and potent in vitro antagonistic activity (IC50=2.18 nM). GnRH-R antagonist 1 can be used in studies of advanced prostate cancer and premature LH peaks preventing .
Cemiplimab (Anti-Human PD-1) is a high-affinity programmed death receptor-1 (PD-1) monoclonal IgG4 antibody that blocks PD-1/PD-L1-mediated T-cell suppression. Cemiplimab is commonly used in squamous cell skin cancer research .
Levocabastine (R 50547) is a potent and selective histamine H1-receptor antagonist. Levocabastine hydrochloride is also a selective, highaffinityneurotensin receptor subtype 2 (NTR2) antagonist, with a Ki of 17 nM for mNTR2. Levocabastine can act as a VLA-4 antagonist, interferes with conjunctival eosinophil infiltration in allergic conjunctivitis (AC) .
(Pro3) GIP, human ((Pro3) Gastric Inhibitory Peptide, human) is an efficacious, stable and specific human GIP receptor (hGIPR) full agonist. (Pro3) GIP, human has high binding affinity for human GIPR with Ki/ Kd values of 0.90 nM. (Pro3) GIP, human can be used for the research of obesity-related diabetes .
Tildrakizumab (SCH 900222) is a humanized anti-IL-23 (p19 subunit) monoclonal antibody. IL-23 is a critical cytokine to maintain the Th17 cell phenotype. Tildrakizumab has high-affinity for single-chain IL-23 (Kd: 136 pM). Tildrakizumab is effective against moderate to severe plaque psoriasis .
Tri-GalNAc-DBCO can bind to the desialic acid glycoprotein receptor (ASGPR) to drive protein downregulation and target protein degradation, where GalNAc is a high-affinity ligand for hepatocyte-specific ASGPR . Tri-GalNAc-DBCO is a click chemistry reagent, it contains a DBCO group that can undergo strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing Azide groups.
KSK67 is a high-affinity dual sigma-2 and histamine H3 receptor antagonist, with Kis of 3.2, 1531, 101 nM for H3 receptor, sigma-1, sigma-2 receptor respectively. KSK67 can be used for research of nociceptive and neuropathic pain .
SB-258585 is a highaffinity ligand for the 5-HT6 receptor. SB-258585 binds highly to a single receptor population in a human cell line that recombines 5-HT6 receptors. SB-258585 can be used to label recombinant and natural 5-HT6 receptor .
Pulcherriminic acid is a cyclic dipeptide antimicrobial agent with highaffinity for Fe 3+, found mainly in Bacillus and yeast. Pulcherriminic acid chelates iron ions through a non-enzymatic reaction to form the extracellular red pigment pulcherrimin, which competes for iron nutrition and thus achieves an antibacterial effect. Pulcherriminic acid has great applications in food, agriculture and medical industries .
BRL-15572 dihydrochloride is a selective antagonist of h5-HT1D, displays highaffinity for h5-HT1D receptors. BRL-15572 dihydrochloride could be useful pharmacological agents to characterise 5-HT1D receptor mediated responses .
MK-2894 is a potent, selective, orally active and highaffinity (Ki=0.56 nM) full antagonist against E prostanoid receptor 4 (EP4 receptor) (IC50=2.5 nM). MK-2894 possesses potent anti-inflammatory activity in animal models of pain/inflammation and can be used for the research of arthritis .
MK-2894 sodium salt is a potent, selective, orally active and highaffinity (Ki=0.56 nM) full antagonist against E prostanoid receptor 4 (EP4 receptor) (IC50=2.5 nM). MK-2894 sodium salt possesses potent anti-inflammatory activity in animal models of pain/inflammation and can be used for the research of arthritis .
AGN 194310 (VTP-194310) is a highaffinity, potent and selective retinioic acid receptors (RARs) pan-antagonist with Kd values of 3 nM, 2 nM, 5 nM for RARα, RARβ, RARγ, respectively . AGN 194310 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
JP1302 dihydrochloride is a potent, selective, highaffinity antagonist of the α2C-adrenoceptor, with a Kb of 16 nM and a Ki of 28 nM for the human α2C-receptor. JP1302 dihydrochloride shows antidepressant and antipsychotic-like effects. JP1302 dihydrochloride can be used for neuropsychiatric disorders and renal dysfunction research .
CS-003 Free base (CS-003), a triple tachykinin receptor antagonist, shows highaffinities for human (Neurokinin) NK1, NK2 and NK3 receptors with Ki values of 2.3 nM, 0.54 nM and 0.74 nM, respectively. CS-003 Free base (CS-003) has therapeutic efficacy on respiratory diseases associated with neurokinins.
DPA-714 is a highaffinity translocator protein (TSPO) ligand (Ki=7 nM), which is designed with a fluorine atom in its structure, allowing labelling with fluorine -18 and in vivo imaging using positron emission tomography. 18FDPA-714 successfully evaluates for the specific imaging of inflammation in various models of neuroinflammation and in a brain tumor model .
EC359 is a potent, selective, highaffinity and orally active leukemia inhibitory factor receptor (LIFR) inhibitor with a Kd of 10.2 nM, which directly interacts with LIFR to effectively block LIF/LIFR interactions . EC359 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
RVD-Hpα TFA is the N-terminally extended form of human hemopressin that acts as a selective CB1 receptor agonist. RVD-Hpα TFA increases intracellular Ca 2+ levels in cells expressing CB1 receptors in vitro. RVD-Hpα TFA also highaffinity CB2 positive allosteric modulator (Ki=50 nM).
SBP-7455 is a potent, highaffinity and orally active dual ULK1/ULK2 autophagy inhibitor with IC50s of 13 nM and 476 nM in the ADP-Glo assays, respectively. SBP-7455 potently inhibits ULK1/2 enzymatic activity and can be used for triple-negative breast cancer (TNBC) research .
BRL-15572 hydrochloride is a selective antagonist of h5-HT1D, displays highaffinity for h5-HT1D receptors. BRL-15572 hydrochloride could be useful pharmacological agents to characterise 5-HT1D receptor mediated responses .
TPP-1 TFA is a potent inhibitor of the PD-1/PD-L1 interaction. TPP-1 TFA binds specifically to PD-L1 with a highaffinity (KD=95 nM). TPP-1 TFA inhibits human tumor growth in vivo via reactivating T-cell function .
Dmt-2'fluoro-da(bz) amidite, an uniformly modified 2'-deoxy-2'-fluoro phosphorothioate oligonucleotide, is a nuclease-resistant antisense compound with highaffinity and specificity for RNA targets. Dmt-2'fluoro-da(bz) amidite is also an intermediate for 5’-DMT-3’-phosphoramidite synthesis .
NS3861 fumarate is an agonist of nicotinic acetylcholine receptors (nAChRs) and binds with highaffinity to heteromeric α3β4 nAChR. The binding Ki values of 0.62, 25, 7.8, 55 nM for α3β4, α3β2, α4β4, α4β2, respectively .
NS3861 is an agonist of nicotinic acetylcholine receptors (nAChRs) and binds with highaffinity to heteromeric α3β4 nAChR. The binding Ki values of 0.62, 25, 7.8, 55 nM for α3β4, α3β2, α4β4, α4β2, respectively .
ERCC1-XPF-IN-1 is a potent and high-affinityERCC1-XPF inhibitor with IC50 value of 0.49 μM. ERCC1-XPF-IN-1 has the capacity to potentiate the cytotoxicity effect of UV radiation and inhibiting DAN repair, by the inhibition of removal of CPDs, and cyclophosphamide toxicity to colorectal cancer cells .
Mazaticol is an anticholinergic agent. Mazaticol blocks the muscarinic acetylcholine receptors and cholinergic nerve activity. Mazaticol is a potent 3H-QNB and 3H-PZ binding inhibitor, can bind to the M2 receptors with highaffinity. Mazaticol exhibits inhibitory effects on dopamine uptake in the striatal nerve terminal. Mazaticol can be used for parkinsonian syndrome research .
Zalutumumab is a highaffinity, completely human IgG1 monoclonal antibody targeting EGFR. Zalutumumab binds to domain III of the EGF receptor and acts by blocking the binding of EGF and by sterically interfering with the active conformation of the receptor. Zalutumumab binds with IgG and its Fab fragment with EC50s of 7 and 19 nM, respectively. Zalutumumab can be used for the research of cancer .
Biotin-PEG-Thiol (MW 2000) is an active compound. Biotin-PEG-Thiol (MW 2000) is pegylated by binding to streptavidin or antibiotin with highaffinity and specificity. Biotin-PEG-Thiol (MW 2000) can modify biomolecules, proteins, peptides and other small molecule materials. Biotin-PEG-Thiol (MW 2000) is widely used in the research of agent release and nano new materials .
Antibacterial agent 130 is a 1,1-diarylthiogalactoside, used for targeting the Pseudomonas aeruginosaLecA. Antibacterial agent 130 shows highaffinity toward LecA (Kd=1 μM). Antibacterial agent 130 has antibiofilm activity, but lacks bactericidal activity. LecA, a lectin and virulence factor from Pseudomonas aeruginosa involved in bacterial adhesion and biofilm formation .
Surzebiclimab (BGB-A425) is a humanized IgG1-variant monoclonal antibody against T-cell immunoglobulin and mucin-domain containing-3 (TIM-3). Surzebiclimab binds to the extracellular domain of human Tim-3 with highaffinity (KD=0.36 nM) and specificity. Surzebiclimab can be used in research of cancer .
JP1302 is a potent, selective, highaffinity antagonist of the α2C-adrenoceptor, with a Kb of 16 nM and a Ki of 28 nM for the human α2C-receptor. JP1302 shows antidepressant and antipsychotic-like effects. JP1302 can be used for neuropsychiatric disorders and renal dysfunction research .
Fura-FF AM is a cell-permeable acetoxymethyl ester of fura-FF, a dluorescent calcium indicator. Fura-FF AM is hydrolyzed by intracellular esterases to release fura-FF in cells. Fura-FF is a difluorinated derivative of the calcium indicator fura-2. Compared to fura-2, fura-FF has a low affinity for calcium and is suitable for studying compartments with high concentrations of calcium.
Samidorphan (ALKS-33) is an orally active opioid system modulator that has a highaffinity for binding with μ‐opioid, κ‐opioid, and δ‐opioid receptors. Samidorphan acts as an antagonist at μ‐opioid receptors and acts as a partial agonist at k-opioid and δ‐opioid receptors. Samidorphan primarily acts as an opioid receptor antagonist in vivo .
CH5138303 is a potent and orally active Hsp90 inhibitor. CH5138303 shows high binding affinity for N-terminal Hsp90α, with Kd of 0.52 nM. CH5138303 shows potent anti-proliferative activity against human cancer cell lines (HCT116 and NCI-N87), with IC50 values of 0.098 and 0.066 μM, respectively. CH5138303 shows high oral bioavailability in mice (F=44.0%). CH5138303 shows potent antitumor efficacy in a human NCI-N87 gastric cancer xenograft model .
Carbetocin, an oxytocin (OT) analogue, is an oxytocin receptor agonist with a Ki of 7.1 nM. Carbetocin has highaffinity to chimeric N-terminus (E1) of the oxytocin receptor (Ki=1.17 μM). Carbetocin has the potential for postpartum hemorrhage research. Carbetocin can crosse the blood-brain barrier and produces antidepressant-like activity via activation of oxytocin receptors in the CNS .
Dagrocorat (PF-00251802) is an orally active and selective high-affinity partial agonist of the glucocorticoid receptor. Dagrocorat is also a time-dependent reversible inhibitor of CYP3A (IC50=1.3 μM in human liver microsomes) and CYP2D6 (Ki=0.57 μM in human liver microsomes). Dagrocorat can be used for the research of rheumatoid arthritis .
TPA-023B is a high-affinity and orally active GABAA receptor α2/α3 subtype (Kis of 0.73 nM/2 nM) partial agonist and a α1 subtype (Ki of 1.8 nM) antagonist. TPA-023B has non-sedating anxiolytic-like properties .
LXW7, a cyclic peptide containing Arg-Gly-Asp (RGD), is an integrin αvβ3 inhibitor. LXW7 has a high binding affinity to αvβ3 integrin with an IC50 of 0.68 μM. LXW7 increases phosphorylation of VEGFR-2 and activation of ERK1/2. Anti-inflammatory effect .
HPV16-E711-20 epitope is a well-known HLA-A *0201-restricted human cytotoxic T lymphocyte (CTL) epitope of the HPV16 E7 protein that shows high-affinity binding to HLA-A2 in vitro. HPV16 CTL epitopes may be good candidates for the development of an effective peptide-based antitumor vaccine .
BRD-6929 is a potent, selective brain-penetrant inhibitor of class I histone deacetylase HDAC1 and HDAC2 inhibitor with IC50 of 1 nM and 8 nM, respectively. BRD-6929 shows high-affinity to HDAC1 and HDAC2 with Ki of 0.2 and 1.5 nM, respectively. BRD-6929 can be used for mood-related behavioral model research .
Danicopan (ACH-4471), a selective and orally active small-molecule factor D inhibitor, shows high binding affinity to human Factor D with Kd value of 0.54 nM. Danicopan (ACH-4471) inhibits alternative pathway of complement (APC) activity, has potential to block the alternative pathway of complement in paroxysmal nocturnal hemoglobinuria (PNH) and atypical hemolytic uremic syndrome (aHUS) .
Reslizumab (Sch 55700) is humanized monoclonal antibodies that target interleukin-5 (IL-5) for the treatment of eosinophilic asthma. Reslizumab is effective in neutralizing the function of IL-5. Reslizumab has high binding affinity for human IL-5, with KD values of 109 pM and 4.3 pM in the the Biacore surface plasmon resonance and Kinetic Exclusion Assay, respectively .
BAY 60-6583 is a potent and high-affinity agonist of adenosine A2B receptor (EC50 = 3 nM) over A1, A2A, and A3 receptors. BAY 60-6583 binds to mouse, rabbit, and dog A2BAR with Ki values of 750 nM, 340 nM and 330 nM, respectively. BAY 60-6583 has a cardioprotective effect in a myocardial ischemia model .
PNU-142633 is a highaffinity, selective and orally active 5-HT1D receptor agonist with Kis of 6 nM and > 18 000 nM for human 5-HT1D receptor and human 5-HT1B receptor, respectively. PNU-142633 has anti-migraine efficacy .
2-Chloroadenosine, a stable adenosine analogue, protects against long term development of ischaemic cell loss in the rat hippocampus. 2-Chloroadenosine is an apparent competitive inhibitor of uridine influx (apparent Ki=33 μM) and high-affinity nitrobenzylthioinosine binding (apparent Ki=0.18 mM). 2-Chloroadenosine is a transported permeant for the nucleoside transporter in human erythrocytes .
Dicyclomine hydrochloride is a potent and orally active muscarinic cholinergic receptors antagonist. Dicyclomine hydrochloride shows highaffinity for muscarinic M1 receptor subtype (Ki=5.1 nM) and M2 receptor subtype (Ki=54.6 nM) in brush-border membrane and basal plasma membranes, respectively . Dicyclomine is an antispasmodic agent and relieves smooth muscle spasm of the gastrointestinal tract in vivo .
CALP2 is a calmodulin (CaM) antagonist ( (Kd of 7.9 µM)) with highaffinity for binding to the CaM EF-hand/Ca 2+-binding site. CALP2 inhibits CaM-dependent phosphodiesterase activity and increases intracellular Ca 2+ concentrations. CALP2 potently inhibits of adhesion and degranulation. CALP2 is also a strong activator of alveolar macrophages .
Sarilumab (Anti-Human IL6Rα, Human Antibody) is a human immunoglobulin G1 monoclonal antibody. Sarilumab, a interleukin-6 (IL-6) receptor antagonist, binds to the IL-6 receptor with highaffinity and inhibits cis and trans signaling by IL-6, resulting in reduced inflammation. Sarilumab can be used for the research of Rheumatoid arthritis .
Apelin-12 is one of the most potent C-terminal fragments of the polypeptide that possesses a highaffinity to orphan receptor APJ receptor. Apelin-12 is involved in the regulation of body fluid homeostasis and in the central control of feeding. Apelin-12 blocks HIV-1 entry through APJ receptor. Apelin-12 exerts neuroprotective effect .
MPP+ iodide, a toxic metabolite of the neurotoxin MPTP, causes symptom of Parkinson's disease in animal models by selectively destroying dopaminergic neurons in substantia nigra. MPP+ iodide is taken up by the dopamine transporter into dopaminergic neurons where it exerts its neurotoxic action on mitochondria by affecting complex I of the respiratory chain. MPP+ iodide is also a highaffinity substrate for the serotonin transporter (SERT) .
Dagrocorat (PF-00251802) hydrochloride is an orally active and selective high-affinity partial agonist of the glucocorticoid receptor. Dagrocorat hydrochloride is also a time-dependent reversible inhibitor of CYP3A (IC50=1.3 μM in human liver microsomes) and CYP2D6 (Ki=0.57 μM in human liver microsomes). Dagrocorat hydrochloride can be used for the research of rheumatoid arthritis .
Carbetocin acetate, an oxytocin (OT) analogue, is an oxytocin receptor agonist with a Ki of 7.1 nM. Carbetocin acetate has highaffinity to chimeric N-terminus (E1) of the oxytocin receptor (Ki=1.17 μM). Carbetocin acetate has the potential for postpartum hemorrhage research. Carbetocin acetate can crosse the blood-brain barrier and produces antidepressant-like activity via activation of oxytocin receptors in the CNS .
Daclizumab (Zenapax) is a humanized, monoclonal antibody that blocks CD25 (α-subunit of the high-affinity interleukin-2 receptor (IL-2R-HA)). Daclizumab (Zenapax) reversibly binds to CD25and prevents the interaction of IL-2 with the IL-2R-HA. Daclizumab (Zenapax) can be used for multiple sclerosis research .
BDA-366 is a potent Bcl2 antagonist (Ki = 3.3 nM), binding Bcl2-BH4 domain with highaffinity and selectivity. BDA-366 induces conformational change in Bcl2 that abrogates its antiapoptotic function, converting it from a survival molecule to a cell death inducer. BDA-366 suppresses growth of lung cancer cells .
cis-α-(Carboxycyclopropyl)glycine (L-CCG III) is a potent, competitive glutamate uptake inhibitor. cis-α-(Carboxycyclopropyl)glycine is a substrate of glutamate transporters (GluT) (EC50: 13 μM, 2 μM for EAAT 1 and EAAT 2, respectively). cis-α-(Carboxycyclopropyl)glycine inhibits a Na +-dependent high-affinity L-glutamate uptake in glial plasmalemmal vesicles (GPV) and synaptosomes .
Abicipar pegol (AGN-150998, MP0112) is an anti-VEGF DARPin molecule, a novel class of small proteins containing ankyrin repeat domains engineered to bind with high specificity and affinity to target proteins. Abicipar pegol effectively inhibits angiogenesis and vascular permeability and is used in the study of diseases related to ocular inflammation by intravitreal injection, reducing mean retinal thickness and leakage area .
Stamulumab (MYO-029) is a recombinant human IgG1λ antibody that binds to myostatin and neutralizes its activity by preventing binding to its endogenous high-affinity receptor ActRIIB. Stamulumab leads to muscle fiber hypertrophy and not hyperplasia in SCID mice. Stamulumab has the potential for Becker muscular dystrophy (BMD), facioscapulohumeral dystrophy (FSHD), and limb-girdle muscular dystrophy (LGMD) research .
BIBO3304 (diTFA) is an orally effective and selective neuropeptide Y (NPY) Y1 receptor antagonist. BIBO3304 (diTFA) has a highaffinity for both human and rat Y1 receptors, with IC50 values of 0.38 and 0.72 nM, respectively. BIBO3304 (diTFA) promotes bone-tendon healing through the Wnt/β-catenin signaling pathway .
PB28 is a cyclohexylpiperazine derivative and a highaffinity and selective sigma 2 (σ2) receptor agonist with a Ki of 0.68 nM. PB28 is also a σ1 antagonist with a Ki of 0.38 nM. PB28 is less affinity for other receptors. PB28 inhibits electrically evoked twitch in guinea pig bladder and ileum with EC50 values of 2.62 μM and 3.96 μM, respectively. PB28 can modulate SARS-CoV-2-human protein-protein interaction. PB28 induces caspase-independent apoptosis and has antitumor activity .
PB28 dihydrochloride, a cyclohexylpiperazine derivative, is a highaffinity and selective sigma 2 (σ2) receptor agonist with a Ki of 0.68 nM. PB28 dihydrochloride is also a σ1 antagonist with a Ki of 0.38 nM. PB28 dihydrochloride is less affinity for other receptors. PB28 dihydrochloride inhibits electrically evoked twitch in guinea pig bladder and ileum with EC50 values of 2.62 μM and 3.96 μM, respectively. PB28 dihydrochloride can modulate SARS-CoV-2-human protein-protein interaction. PB28 dihydrochloride induces caspase-independent apoptosis and has antitumor activity .
BLM-IN-1 is an effective bloom syndrome protein (BLM) inhibitor. BLM-IN-1 has a high binding affinity with a KD valueof 1.81 μM. BLM-IN-1 has good inhibitory effect for BLM with an IC50 value of 0.95 μM. BLM-IN-1 can induce cell apoptosis. BLM-IN-1can be used for the research of DNA damage and cancer .
BMS-986020 (AM152) sodium is a high-affinity lysophosphatidic acid receptor 1 (LPA1) antagonist . BMS-986020 sodium inhibits bile acid and phospholipid transporters with IC50s of 4.8 µM, 6.2 µM, and 7.5 µM for BSEP, MRP4, and MDR3, respectively . BMS-986020 sodium has the potential for the treatment of idiopathic pulmonary fibrosis (IPF) .
Shield-1 (Shld1) is a specific, cell-permeant and high-affinity ligand of FK506-binding protein-12 (FKBP), and reverses the instability by binding to mutated FKBP (mtFKBP), allowing conditional expression of mtFKBP-fused proteins. Shield-1 can stabilize proteins tagged with a mutated FKBP12-derived destabilization domain (DD) .
LXW7 TFA, a cyclic peptide containing Arg-Gly-Asp (RGD), is an integrin αvβ3 inhibitor. LXW7 has a high binding affinity to αvβ3 integrin with an IC50 of 0.68 μM. LXW7 TFA increases phosphorylation of VEGFR-2 and activation of ERK1/2. Anti-inflammatory effect .
K-(D-1-Nal)-FwLL-NH2 TFA is a highaffinity and potent ghrelin receptor inverse agonist (Ki values are 4.9 and 31 nM in COS7 and HEK293T cells, respectively). K-(D-1-Nal)-FwLL-NH2 blocks ghrelin receptor-mediated Gq- and G13-dependent signaling pathways.
1-Oleoyl lysophosphatidic acid (1-Oleoyl-sn-glycero-3-phosphate) is an abundant lysophosphatidic acid (LPA) species with high biological activity due to its strong affinity for the LPA receptors. 1-Oleoyl lysophosphatidic acid is commonly used in most laboratories as a reagent for LPA receptor activation . 1-Oleoyl lysophosphatidic acid increases SRE-driven β-galactosidase activity .
BMS-604992 (EX-1314) free base is a selective, orally active small-molecule growth hormone secretagogue receptor (GHSR) agonist. BMS-604992 free base demonstrates high-affinity binding (ki=2.3 nM) and potent functional activity (EC50=0.4 nM). BMS-604992 free base can stimulate food intake in rodents .
JNJ-54717793, as a brain penetrant, is an orally active, selective and highaffinityorexin-1 receptor (OX1R) antagonist (plasma EC50=85 ng/mL). The Ki values of JNJ-54717793 for hOX1R (human OX1R) and hOX2R are 16 nM and 700 nM, respectively. JNJ-54717793 is a potent compound of anxiety disorders .
cis-Urocanic acid- 13C3 is the 13C-labeled cis-Urocanic acid. cis-Urocanic acid is a 5-HT2A receptor agonist. cis-Urocanic acid binds to 5-HT receptor with relatively highaffinity (Kd=4.6 nM). cis-Urocanic acid is an immune modulator that induces immunosuppression by binding to the 5-HT2A receptor[1].
Barnidipine-d5 (hydrochloride) is the deuterium labeled Barnidipine hydrochloride. Barnidipine hydrochloride (Mepirodipine hydrochloride) is an L-type calcium antagonist (CaA) with highaffinity for [3H] initrendipine binding sites (Ki=0.21 nmol/l), has selective action against CaA receptors[1].Barnidipine hydrochloride (Mepirodipine hydrochloride) is an antihypertensive agent and acts by the reduction of peripheral vascular resistance secondary to its vasodilatory action[2].
MA242 free base is a specific dual inhibitor of MDM2 and NFAT1. MA242 free base directly binds both MDM2 and NFAT1 with highaffinity, induces their protein degradation, and inhibits NFAT1-mediated transcription of MDM2. MA242 free base induces apoptosis in pancreatic cancer cell lines regardless of p53 status .
Dicyclomine (Dicycloverine) is a potent and orally active muscarinic cholinergic receptors antagonist. Dicyclomine (Dicycloverine) shows highaffinity for muscarinic M1 receptor subtype (Ki=5.1 nM) and M2 receptor subtype (Ki=54.6 nM) in brush-border membrane and basal plasma membranes, respectively . Dicyclomine is an antispasmodic agent and relieves smooth muscle spasm of the gastrointestinal tract in vivo .
MAGLi 432 is a non-covalent, potent, highly selective, and reversible MAGL inhibitor. MAGLi 432 binds with highaffinity to the MAGL active site, with IC50 values of 4.2 nM (human enzyme) and 3.1 nM (mouse enzyme). MAGLi 432 can be used in the research of chronic inflammation, blood–brain barrier dysfunction, neurological disorders such as multiple sclerosis, Alzheimer’s disease and Parkinson’s disease .
CYP3A4-IN-3 is a high-affinity specific inhibitor of cytochrome P450 3A4 (CYP3A4) with the IC50 value of 0.075 μM. CYP3A4-IN-3 is a ritonavir analogue, but with a simpler structure and twice the inhibitory effect of ritonavir. CYP3A4-IN-3 is used as an antiviral agent and immunosuppressant .
Emactuzumab(RG 7155) is a specific monoclonal antibody that inhibits colonystimulating factor 1 receptor (CSF1R) activation. Emactuzumab has highaffinity for CSF-1R with Ki value of 0.2 nM to blocks CSF-1R dimerization. Emactuzumab can be used for the research of several diseases, such as diffuse-type tenosynovial giant cell tumour (dt-GCT) .
TSR-033 is a highaffinity human IgG4 antibody targeting LAG-3 (lymphocyte activation gene-3), a co-receptor associated with impaired T cell function and often co-expressed with PD-1, that enhances T cell function and PD-1 blocking activity in vitro and in vivo. TSR-033 has anti-tumor activity .
Antitumor agent-87 is a potent antitumor agent. Antitumor agent-87 shows a highaffinity for CYP1A1 with a Ki value of 0.23 µM. Antitumor agent-87 shows antiproliferative activity. Antitumor agent-87 induces cell cycle arrest at the G2/M phase. Antitumor agent-87 show antitumoral activity .
GZ-11608 is a potent and selective vesicular monoamine transporter-2 (VMAT2) inhibitor with highaffinity (Ki = 25 nM). GZ-11608 decreases methamphetamine-induced dopamine release from isolated synaptic vesicles from brain dopaminergic neurons. GZ-11608 exhibits rapid brain penetration and without neurotoxicity. GZ-11608 can be used for the research of methamphetamine use disorder .
AR-A 2 is a selective 5-HT1B receptor antagonist, with highaffinity to guinea pig cortex 5HT1B/1D and recombinant guinea pig 5-HT1B receptors (Ki=0.24 and 0.47 nM) and with 10-fold lower affinity to guinea pig 5-HT1D receptor (Ki, 5 nM), and shows an EC50 of 4.5 nM for the guinea pig 5-HT1B receptor; AR-A 2 can be used in the research of depression and anxiety.
BMS-986020 (AM152) is a high-affinity and selective lysophosphatidic acid receptor 1 (LPA1) antagonist . BMS-986020 inhibits bile acid and phospholipid transporters with IC50s of 4.8 µM, 6.2 µM, and 7.5 µM for BSEP, MRP4, and MDR3, respectively . BMS-986020 has the potential for the treatment of idiopathic pulmonary fibrosis (IPF) .
Evans Blue (Direct Blue 53) is a potent inhibitor of L-glutamate uptake via the membrane bound excitatory amino acid transporter (EAAT). Evans Blue is a L-glutamate and kainate receptor-mediated currents inhibitor. Evans Blue has a strong affinity towards serum albumin, making it a high molecular weight protein tracer. Evans Blue is also used to study BBB (blood-brain barrier) permeability .
JNJ-39758979 is a selective, orally active, and high-affinityhistamine H4 receptor antagonist with Kis of 12.5, 5.3, and 25 nM for human, mouse, and monkey histamine H4 receptor, respectively. JNJ-39758979 functionally antagonizes histamine-induced cAMP inhibition with a pA2 of 7.9 in transfected cells. JNJ-39758979 shows good anti-inflammatory and antipruritic activity .
DB1976 is a selenophene analog of DB270 and a potent and cell-permeable fully efficacious transcription factor PU.1 inhibitor. DB1976 potently inhibits PU.1 binding (IC50 of 10 nM) and strongly inhibits the PU.1/DNA complex (with high DB1976-λB affinity, KD of 12 nM) in vitro. DB1976 has apoptosis-inducing effect .
Sigma‑1 receptor antagonist 1 (compound 137) is a potent and selective sigma-1 receptor (σ1R) antagonist, with a high binding affinity to σ1R receptor (Ki = 1.06 nM). Sigma‑1 receptor antagonist 1 exhibits antineuropathic pain activity and acts as a promising agent for the treatment of neuropathic pain .
DB1976 dihydrochloride is a selenophene analog of DB270 and a potent and cell-permeable fully efficacious transcription factor PU.1 inhibitor. DB1976 dihydrochloride potently inhibits PU.1 binding (IC50 of 10 nM) and strongly inhibits the PU.1/DNA complex (with high DB1976-λB affinity, KD of 12 nM) in vitro. DB1976 dihydrochloride has apoptosis-inducing effect .
CALP2 TFA is a calmodulin (CaM) antagonist (Kd of 7.9 µM) with highaffinity for binding to the CaM EF-hand/Ca 2+-binding site. CALP2 TFA inhibits CaM-dependent phosphodiesterase activity and increases intracellular Ca 2+ concentrations. CALP2 TFA potently inhibits of adhesion and degranulation. CALP2 TFA is also a strong activator of alveolar macrophages .
JNJ-39758979 dihydrochloride is a selective, orally active, and high-affinityhistamine H4 receptor antagonist, with Kis of 12.5, 5.3, and 25 nM for human, mouse, and monkey histamine H4 receptor, respectively. JNJ-39758979 dihydrochloride functionally antagonizes histamine-induced cAMP inhibition with a pA2 of 7.9 in transfected cells. JNJ-39758979 dihydrochloride shows good anti-inflammatory and antipruritic activity .
3-Chlorodiphenylamine is a highaffinityCa 2+ sensitizer of cardiac muscle. 3-Chlorodiphenylamine is based on diphenylamine and binds to the isolated N-domain of cardiac troponin C (cTnC) (Kd=6 µM). 3-Chlorodiphenylamine is an excellent starting scaffold for the development of more potent Ca 2+-sensitizing compounds due to its small size, and can be used for systolic heart failure research .
Toluidine Blue (Toluidine Blue O) is an alkaline quinonimine dye (vivo dye) with highaffinity for acidic tissue components, staining nuclei blue and polysaccharides purple. Toluidine Blue shows heterostaining properties for mast cells, mucins and chondrocytes. Toluidine Blue can stain different components of plant tissues and cells in different colours. Toluidine Blue is also used as a diagnostic aid to identify malignant lesions, such as cancer .
JNJ-26070109 is a high-affinity, competitive, orally bioactive, and selective cholecystokinin 2 (CCK2) receptor antagonist with good pharmacokinetic properties, with pKis of 8.49, 7.99, and 7.70 for human, rat, and dog CCK2 receptors, respectively. The dual function of CCK2 receptors in regulating gastric acid secretion and growth of the gastrointestinal mucosa make this an attractive and novel target for the research of gastroesophageal reflux disease .
Desmethylazelastine is a main active metabolite of Azelastine that is oxidatively metabolized by the cytochrome P450 enzyme system with a protein binding rate of 97% and an elimination half-life of 54 hours. Azelastine is an orally active, selective and high-affinityhistamine H1-receptor antagonist. Azelastine can be used in studies of allergic rhinitis, asthma, diabetic hyperlipidemic and SARS-CoV-2 .
Clozapine (HF 1854) is an antipsychotic used for the research of schizophrenia. Clozapine has highaffinity for a number of neuroreceptors. Clozapine is a potent antagonist of dopamine D2 with a Ki of 75 nM. Clozapine inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor with Kis of 9.5 nM and 4 nM, respectively . Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM) .
Ensaculin free base (KA-672) is a NMDA antagonist and have highaffinities to serotonergic 5-HT1A and 5-HT7 receptors, adrenergic α1, and dopaminergic D2 and D3 receptors. Ensaculin free base is a memory-enhancing agent. Ensaculin free base has the potential as an antidementia agent acting on various transmitter systems .
HS-291 is a HtpG inhibitor of Borrelia burgdorferi (Bb). HS-291 contains BX-2819 (highaffinity for Bb HtpG), PEG linker, and Verteporfin (HY-B0146) (a photoactive toxin).HS-291 produces reactive oxygen species under light activation to oxidize HtpG and a discrete protein subset near chaperone proteins and can quickly and irreversibly inactivate Bb .
Dihexa, an oligopeptide drug, is an orally active and blood-brain barrier-permeable angiotensin IV analog. Dihexa binds to hepatocyte growth factor (HGF) with highaffinity (Kd=65 pM) and potentiates its activity at its receptor, c-Met. Dihexa exhibits excellent antidementia activity and improves cognitive function in animal models. Dihexa may have therapeutic potential as a treatment Alzheimer’s disease .
SCH-23390 hydrochloride (R-(+)-SCH-23390 hydrochloride) is a potent and selective dopamine D1-like receptor antagonist with Kis of 0.2 nM and 0.3 nM for the D1 and D5 receptor, respectively. SCH-23390 hydrochloride is a potent and high efficacy human 5-HT2C receptor agonist with a Ki of 9.3 nM. SCH-23390 hydrochloride also binds with highaffinity to the 5-HT2 and 5-HT1C receptors. SCH-23390 hydrochloride inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with an IC50 of 268 nM .
SCH-23390 maleate (R-(+)-SCH-23390 maleate) is a potent and selective dopamine D1-like receptor antagonist with Kis of 0.2 nM and 0.3 nM for the D1 and D5 receptor, respectively. SCH-23390 maleate is a potent and high efficacy human 5-HT2C receptor agonist with a Ki of 9.3 nM. SCH-23390 maleate also binds with highaffinity to the 5-HT2 and 5-HT1C receptors. SCH-23390 maleate inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with an IC50 of 268 nM .
Propranolol hydrochloride is a nonselective β-adrenergic receptor (βAR) antagonist, has highaffinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively . Propranolol hydrochloride inhibits [ 3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM . Propranolol hydrochloride is used for study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy .
Propranolol is a nonselective β-adrenergic receptor (βAR) antagonist, has highaffinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively . Propranolol inhibits [ 3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM . Propranolol is used for the study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy .
Margatoxin, an alpha-KTx scorpion toxin, is a highaffinity inhibitor of Kv1.3 (Kd=11.7 pM). Margatoxin inhibits the Kv1.2 (Kd=6.4 pM) and Kv1.1 (Kd=4.2 nM). Margatoxin, a 39 amino-acid-long peptide, is isolated from the venom of the scorpion Centruroides margaritatus and widely used in ion channel research .
GABAA receptor agent 2 TFA is a potent and high-affinityGABAA receptor antagonist with an IC50 of 24 nM (human α1β2γ2 GABAA-expressing tsA201 cells) and a Ki of 28 nM (rat GABAA receptors). GABAA receptor agent 2 TFA is inactive against four human GABA transporters (hGAT-1, hBGT-1, hGAT-2, and hGAT-3) .
SEN 12333 (WAY-317538) is a potent, selective and orally active α7 nAChR agonist. SEN12333 displays highaffinity for the rat α7 nAChRs expressed in GH4C1 cells (K>i=260 nM) and acts as full agonist in functional Ca 2+ flux studies (EC50=1.6 μM). SEN 12333 is used for AD and schizophrenia research .
Dyrk1A-IN-3 (Compound 8b), a highly selective dual-specificity tyrosine-regulated kinase 1A (DYRK1A) inhibitor, maintains high levels of DYRK1A binding affinity (IC50=76 nM). Dyrk1A-IN-3 can be used for the research of neurodegenerative disorders such as Alzheimer’s Disease, Huntington’s Disease, and Parkinson’s Disease .
Coppersensor-1 (CS1) is a membrane-permeable fluorescent dye. Coppersensor-1 has a picomolar affinity for Cu + with high selectivity over competing cellular metalions. Coppersensor-1 as a probe, can selective and sensitive detection of copper(I) ions (Cu +) in biological samples, including live cells. Coppersensor-1 can be used for the research of imaging of severe diseases such as cancer, cardiovascular disorders and neurogenerative diseases .
Nefazodone is an orally active phenylpiperazine antidepressant. Nefazodone can potently and selectively block postsynaptic 5-HT2A receptors, and moderately inhibit 5-HT and noradrenaline reuptake. Nefazodone can also relieve the adverse effects of stress on the the immune system of mice. Nefazodone has a highaffinity for CYP3A4 isoenzyme, which indicates that it has certain risk of agent-agent interaction .
Suvratoxumab (MEDI4893) is a long-acting, high-affinityhuman anti-α-toxin monoclonal antibody (IgG1κ type). Suvratoxumab potently neutralizes α-toxin, a key S. aureus virulence factor. Suvratoxumab improves survival and reduces lung injury in an immunocompromised mice model of pneumonia. Suvratoxumab also enhances the antibacterial activity of Vancomycin (HY-B0671) or Linezolid (HY-10394) .
CB2R agonist 1 is a selective ligand of cannabinoid receptor subtype 2 (CB2R) with an EC50 value of 0.56 µM. CB2R agonist 1 has highaffinity and excellent selectivity for human CB2R and CB1R respectively. CB2R agonist 1 regulates the production of pro-inflammatory cytokines and anti-inflammatory cytokines and play an immunomodulatory role .
KRAS inhibitor-3 is an inhibitor of KRAS inhibitor. KRAS inhibitor-3 binds to WT and oncogenic KRAS mutants with highaffinity (KD: 0.28 μM for KRAS WT, 0.63 μM for KRAS G12C, 0.37 μM for KRAS G12D, 0.74 μM for KRAS Q61H). KRAS inhibitor-3 also disrupts interaction of KRAS with Raf .
Cosibelimab (CK-301; TG-1501) is a high-affinity, fully human PD-L1-blocking monoclonal antibody that binds PD-L1 and blocks its interaction with PD-1. Cosibelimab has a functional Fc domain and is capable of inducing ADCC and complement-dependent cytotoxicity (CDC)-mediated killing of PD-L1 + cell lines, including lymphoma cells .
Nebivolol (hydrochloride) (Standard) is the analytical standard of Nebivolol (hydrochloride). This product is intended for research and analytical applications. Nebivolol (R 065824) hydrochloride is an orally active beta receptor blocker and has the high beta(1)-receptor affinity.Nebivolol hydrochloride has direct vasodilator properties and adrenergic blocking characteristics. Nebivolol hydrochloride can be used for the research of kinds of diseases such as hypertension, coronary artery disease, congestive heart failure and ischemic heart disease .
OICR-9429 is highaffinityWD repeat domain 5 (WDR5) inhibitor, competitively blocks WDR5 interaction with MLL protein via binding the central peptide-binding pocket of WDR5. OICR-9429 can suppress histone H3K4 trimethylation and can be used for the research of various cancers including non-MLL-rearranged leukaemia, colon, pancreatic, prostate cancer and bladder cancer (BCa) .
Orexin A (human, rat, mouse) (Hypocretin-1 (human, rat, mouse)), a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A (human, rat, mouse) is a specific, high-affinity agonist for G-protein-coupled receptor OX1R. Orexin A (human, rat, mouse) has a role in the regulation of feeding behavior. Orexin A (human, rat, mouse) is an effective anti-nociceptive and anti-hyperalgesic agent in mice and rats .
PPTN is a potent, high-affinity, competitive and highly selective P2Y14 receptor antagonist with a KB value of 434 pM. PPTN exhibits no agonist or antagonist effect at the P2Y1, P2Y2, P2Y4, P2Y6, P2Y11, P2Y12, or P2Y13 receptors. Anti-inflammatory and immune activity .
HJB97 is a high-affinityBET inhibitor with Kis of 0.9 nM (BRD2 BD1), 0.27 nM (BRD2 BD2), 0.18 nM (BRD3 BD1), 0.21 nM (BRD3 BD2), 0.5 nM (BRD4 BD1), 1.0 nM (BRD4 BD2), respectively. HJB97 is employed for the design of potential PROTAC BET degrader and has antitumor activity .
CF53 is a highly potent, selective and orally active inhibitor of BET protein, with a Ki of <1 nM, Kd of 2.2 nM and an IC50 of 2 nM for BRD4 BD1. CF53 binds to both the BD1 and BD2 domains of BRD2, BRD3, BRD4, and BRDT BET proteins with highaffinities, very selective over non-BET bromodomain-containing proteins. CF53 shows potent anti-tumor activity both in vitro and in vivo .
SB 243213 hydrochloride is an orally active, selective and high-affinity5-HT2C receptor antagonist with a pKi of 9.37 and a pKb of 9.8 for human 5-HT2C receptor. SB 243213 hydrochloride shows greater than a 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels. SB 243213 hydrochloride has improved anxiolytic profile and has the potential for schizophrenia and motor disorders .
SPR inhibitor 3 (SPRi3) is a potent sepiapterin reductase (SPR) inhibitor. SPR inhibitor 3 (SPRi3) displays high binding affinity to human SPR in a cell-free assay (IC50=74 nM) and efficiently reduces biopterin levels in a cell-based assay (IC50=5.2 μM). SPR inhibitor 3 (SPRi3) reduces neuropathic and inflammatory pain through a reduction of BH4 levels .
SB 243213 dihydrochloride is an orally active, selective and high-affinity5-HT2C receptor antagonist with a pKi of 9.37 and a pKb of 9.8 for human 5-HT2C receptor. SB 243213 dihydrochloride shows greater than a 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels. SB 243213 dihydrochloride has improved anxiolytic profile and has the potential for schizophrenia and motor disorders .
Butyrolactone 3 (MB-3) is a specifical small-molecule inhibitor of the histone acetyltransferase Gcn5 (IC50=100 μM), which has a highaffinity to the Gcn5 enzyme comparable to that of its natural substrate, histone H3. Butyrolactone 3 shows weak inhibitory on CBP (IC50=0.5 mM). Butyrolactone 3 can be used in studies of cancer, metabolic, autoimmune and neurological diseases .
DI-591 is a potent, high-affinity and cell-permeable inhibitor of the DCN1-UBC12 interaction. DI-591 binds to DCN1 and DCN2 with Ki values of 12 nM and 10.4 nM, respectively and has no appreciable binding to DCN3, DCN4, and DCN5 proteins. DI-591 selectively inhibits neddylation of cullin 3 but has no or minimal effect on neddylation of other cullin family members .
OPC-14523 hydrochloride is an orally active sigma and 5-HT1A receptor agonist, with highaffinity for sigma receptors (σ1/2 IC50=47/56 nM), the 5-HT1A receptor (IC50=2.3 nM), and the 5-HT transporter (IC50=80 nM). OPC-14523 hydrochloride shows antidepressant-like activity .
Ac-Tyr(PO3H2)-Glu-Glu-Ile-Glu-OH (compound 1) is a high-affinity pentapeptide to bind to the src SH2 domain (IC50≈1 µM). Ac-Tyr(PO3H2)-Glu-Glu-Ile-Glu-OH is an inhibitor for src SH3-SH2:phosphoprotein interactions .
SB 243213 is an orally active, selective and high-affinity5-HT2C receptor antagonist with a pKi of 9.37 and a pKb of 9.8 for human 5-HT2C receptor. SB 243213 shows greater than a 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels. SB 243213 has improved anxiolytic profile and has the potential for schizophrenia and motor disorders .
SB-612111 is a novel and potent opiate receptor-like orphan receptor (ORL-1) antagonist with a highaffinity for hORL-1 (Ki=0.33 nM). SB-612111 exhibits selectivity for μ-, κ- and δ-receptors with Ki values of 57.6 nM, 160.5 nM and 2109 nM, respecticely. SB-612111 effectively antagonizes the pronociceptive action of Nociceptin (HY-P0183) in an acute pain model .
(R)-JNJ-31020028 is a highaffinity, selective brain penetrant neuropeptide Y Y2 receptor antagonist, with pIC50 values of 8.07, 8.22 and 8.21 for human, rat, and mouse Y2 receptor, respectively. (R)-JNJ-31020028 shows >100-fold selective versus human Y1, Y4, and Y5 receptors. (R)-JNJ-31020028 has antidepressant like effects .
PPTN hydrochloride is a potent, high-affinity, competitive and highly selective P2Y14 receptor antagonist with a KB value of 434 pM. PPTN hydrochloride exhibits no agonist or antagonist effect at the P2Y1, P2Y2, P2Y4, P2Y6, P2Y11, P2Y12, or P2Y13 receptors. Anti-inflammatory and anti-immune activity .
UMI-77-d4 is the deuterium labeled UMI-77. UMI-77 is a selective Mcl-1 inhibitor, which shows high binding affinity to Mcl-1 (IC50=0.31 μM). UMI-77 binds to the BH3 binding groove of Mcl-1 with Ki of 490 nM, showing selectivity over other members of anti-apoptotic Bcl-2 members.
Ispronicline (TC-1734), an orally active, brain-selective α4β2 nicotine acetylcholine receptor (nAChR) partial agonist, has shown memory-enhancing properties in rodents and a good tolerability profile. Ispronicline binds to the α4β2 nAChR with highaffinity (Ki=11 nM) and is highly selective to other nAChRs such as α7 nAChR and α3β4 nAChR .
ABT-384 is a potent, selective 11-β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor. ABT-384 exhibits highaffinity (Ki 0.1-2.7 nM) against rodent, monkey, and human 11β-HSD1. ABT-384 blocks regeneration of active cortisol. ABT-384 can be used for the research of Alzheimer’s disease (AD) .
SB-612111 hydrochloride hydrochloride is a novel and potent opiate receptor-like orphan receptor (ORL-1) antagonist with a highaffinity for hORL-1 (Ki=0.33 nM). SB-612111 hydrochloride exhibits selectivity for μ-, κ- and δ-receptors with Ki values of 57.6 nM, 160.5 nM and 2109 nM, respecticely. SB-612111 hydrochloride effectively antagonizes the pronociceptive action of Nociceptin (HY-P0183) in an acute pain model .
Propafenone (SA-79), a sodium-channel blocker, acts an antiarrhythmic agent. Propafenone also has highaffinity for the β receptor (IC50=32 nM) . Propafenone blocks the transient outward current (Ito) and the sustained delayed rectifier K current (Isus) with IC50 values of 4.9 μm and 8.6 μm, respectively . Propafenone suppresses esophageal cancer proliferation through inducing mitochondrial dysfunction and induce apoptosis .
DMA-135 hydrochloride inhibits enterovirus 71 (EV71) IRES-dependent translation and replication. DMA-135 hydrochloride binds to enterovirus 71 (EV71) SLII domain with moderately highaffinity (KD= 520 nM). DMA-135 hydrochloride has no significant toxicity in cell-based studies . DMA-135 (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
MPP+-d3 (iodide) is deuterium labeled MPP+ (iodide). MPP+ iodide, a toxic metabolite of the neurotoxin MPTP, causes symptom of Parkinson's disease in animal models by selectively destroying dopaminergic neurons in substantia nigra. MPP+ iodide is taken up by the dopamine transporter into dopaminergic neurons where it exerts its neurotoxic action on mitochondria by affecting complex I of the respiratory chain. MPP+ iodide is also a highaffinity substrate for the serotonin transporter (SERT)[1][2].
AChE-IN-14 (compound 5) is a potent cholinesterase inhibitor with IC50s of 0.46 , 0.48, and 0.44 μM for electric eel acetylcholinesterase (eeAChE), human recombinant acetylcholinesterase (hAChE), and equine serum butyrylcholinesterase (eqBuChE), respectively. AChE-IN-14 exhibits highaffinity toward human H3 receptor (H3R; Ki= 159.8 nM). AChE-IN-14 can be used for the research of Alzheimer’s disease .
AM8936 acts as a balanced and potent cannabinoid receptor type-1 (CB1) agonist in functional assays (EC50s of 8.6 and 1.4 nM for rCB1 and hCB1, respectively). AM8936 exhibits highaffinity for rat CB1 (rCB1) with Ki of 0.55 nM. AM8936 is a potent and efficacious CB1 agonist in vivo. AM8936 can be used for the research of CNS and metabolic disorders, pain, glaucoma, etc .
BU224 hydrochloride is a selective and highaffinityimidazoline I2 receptor ligand, with a Ki of 2.1 nM. BU224 hydrochloride is sometimes used as an I2 receptor antagonist. BU224 hydrochloride exerts neuroprotective effects, with anti-inflammatory and anti-apoptotic properties. BU224 hydrochloride improves memory in 5XFAD mice, enlarging dendritic spines and reducing Aβ-induced changes in NMDARs. BU224 hydrochloride can be used for Alzheimer's disease research .
Cyclo(Arg-Gly-Asp-D-Phe-Cys) (Cyclo RGDfC), a cyclic RGD peptide which has highaffinity to αvβ3, can disrupt cell integrin interactions. Cyclo(Arg-Gly-Asp-D-Phe-Cys) inhibits pluripotent marker expression in embryonic stem cells (ESCs) and the tumorigenic potential of mESCs in vivo. Cyclo(Arg-Gly-Asp-D-Phe-Cys) can be used in the research of tumors .
Cyclo(Arg-Gly-Asp-D-Phe-Cys) (Cyclo RGDfC) TFA, a cyclic RGD peptide which has highaffinity to αvβ3, can disrupt cell integrin interactions. Cyclo(Arg-Gly-Asp-D-Phe-Cys) TFA inhibits pluripotent marker expression in embryonic stem cells (ESCs) and the tumorigenic potential of mESCs in vivo. Cyclo(Arg-Gly-Asp-D-Phe-Cys) TFA can be used in the research of tumors .
2,4-Difluorophenylethynylcobalamin is a potential B12 antivitamin via binding to human B12 -processing enzyme CblC with highaffinity (KD=130 nm). 2,4-Difluorophenylethynylcobalamin withstood tailoring by CblC, and stabilizes the ternary complex with the cosubstrate glutathione (GSH) . 2,4-Difluorophenylethynylcobalamin is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Margatoxin TFA, an alpha-KTx scorpion toxin, is a highaffinity inhibitor of Kv1.3 (Kd=11.7 pM). Margatoxin TFA inhibits the Kv1.2 (Kd=6.4 pM) and Kv1.1 (Kd=4.2 nM). Margatoxin TFA, a 39 amino-acid-long peptide, is isolated from the venom of the scorpion Centruroides margaritatus and widely used in ion channel research .
Barnidipine-d5 is the deuterium-labeled Barnidipine (HY-107322A). Barnidipine-d5 (Mepirodipine) is an L-type calcium antagonist (CaA) with highaffinity for [ 3H] initrendipine binding sites (Ki=0.21 nmol/l), has selective action against CaA receptors . Barnidipine-d5 (Mepirodipine) is an antihypertensive agent and acts by the reduction of peripheral vascular resistance secondary to its vasodilatory action .
(R)-Citalopram oxalate is an anticonvulsant, antidepressant and muscle relaxant. (R)-Citalopram oxalate is at least 20-fold weaker than S-citalopram (Escitalopram; HY-14258) as inhibitor of the 5-HT transporter (SERT). (R)-Citalopram oxalate functionally antagonises S-citalopram in vivo and in vitro. (R)-Citalopram oxalate has an effect on the association of Escitalopram with the highaffinity primary site, and on its dissociation from the 5-HT transporter, via an allosteric mechanism .
Thyroid hormone receptor antagonist (1-850) is a competitive, selective and high-affinitythyroid hormone receptor (TR) antagonist with an IC50 of 1.5 μM for antagonizing the effect of T3 on TR. Thyroid hormone receptor antagonist (1-850) blocks T3-mediated interaction of TRα and TRβ with nuclear receptor coactivator. Thyroid hormone receptor antagonist (1-850) has no effect on the activity of RARα .
Ozanimod (RPC-1063), a sphingosine 1-phosphate (S1P) receptor modulator that binds with highaffinity selectively to S1P receptor subtypes 1 (S1P1) and 5 (S1P5). Ozanimod has modulate effect for hS1P1 and hS1P5 receptor with EC50s of 1.03 nM and 8.6 nM, respectively. Ozanimod can be used for the research of relapsing multiple sclerosis (MS) .
Relugolix (TAK-385) is a potent, orally active, nonpeptidic gonadotropin-releasing hormone (GnRH) antagonist. Relugolix possesses highaffinity and potent antagonistic activity for human receptor (binding IC50=0.33 nM) and monkey receptor (IC50=0.32 nM) compared with TAK-013 (HY-100209) . Relugolix is used for the study of sex-hormone-dependent diseases, such as including endometriosis, uterine fibroids and prostate cancer et al .
Rhod-2 is a high-affinity visible light excitation wavelength Ca 2+ fluorescent probe, Rhod-2, AM is an acetyl methyl ester derivative of Rhod-2, which has cell membrane permeability and can easily enter cells with simple culture. Once it enters the cell, it is sheared by its lactesterase to produce Rhod-2 without membrane permeability, which remains in the cell to perform the corresponding physiological functions. Maximum excitation/emission wavelength: 549/578 nm .
Orexin A (human, rat, mouse) (Hypocretin-1 (human, rat, mouse)) TFA, a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A (human, rat, mouse) TFA is a specific, high-affinity agonist for G-protein-coupled receptor OX1R. Orexin A (human, rat, mouse) TFA has a role in the regulation of feeding behavior. Orexin A (human, rat, mouse) TFA is an effective anti-nociceptive and anti-hyperalgesic agent in mice and rats .
GS-6201 (CVT-6883) is a selective adenosine A2B receptor antagonist. GS-6201 displays highaffinity and selectivity for the human adenosine A2B receptors (Ki=22 nM) . GS-6201 reduces caspase-1 activity in the heart, and attenuates cardiac remodeling after acute myocardial infarction (AMI) in the mouse . GS-62013 attenuates the airway reactivity induced by NECA, AMP, or allergen in sensitized mice .
pm26TGF-β1 peptide is a peptide that mimics a portion of the human TGF-β1 molecule. pm26TGF-β1 peptide shows highaffinity for the TGF-β1 receptor. pm26TGF-β1 peptide displays potent anti-inflammatory properties and does not exhibit neutrophils’ chemoattraction .
pm26TGF-β1 TFA peptide is a peptide that mimics a portion of the human TGF-β1 molecule. pm26TGF-β1 peptide TFA shows highaffinity for the TGF-β1 receptor. pm26TGF-β1 peptide TFA displays potent anti-inflammatory properties and does not exhibit neutrophils’ chemoattraction .
OPC-14523 free base is an orally active sigma and 5-HT1A receptor agonist, with highaffinity for sigma receptors (σ1/2 IC50=47/56 nM), the 5-HT1A receptor (IC50=2.3 nM), and the 5-HT transporter (IC50=80 nM). OPC-14523 free base shows antidepressant-like activity .
GR231118, an analogue of the C-terminus of neuropeptide Y, is a potent , competitive and relative seletive antagonist at human neuropeptide Y Y receptor with a pKi of 10.4. GR231118 a potent agonist at the human neuropeptide Y Y4 receptor (pEC50=8.6; pKi=9.6) and a weak agonist at the human and rat neuropeptide YY2 and Y5 receptors. GR231118 also has highaffinity for the mouse neuropeptide Y Y6 receptor (pKi= 8.8) .
GR231118 TFA, an analogue of the C-terminus of neuropeptide Y, is a potent , competitive and relative seletive antagonist at human neuropeptide YY receptor with a pKi of 10.4. GR231118 a potent agonist at the human neuropeptide YY4 receptor (pEC50=8.6; pKi=9.6) and a weak agonist at the human and rat neuropeptide Y Y2 and Y5 receptors. GR231118 also has highaffinity for the mouse neuropeptide YY6 receptor (pKi= 8.8) .
Ac-Tyr(PO3H2)-Glu-Glu-Ile-Glu-OH TFA (compound 1) is a high-affinity pentapeptide to bind to the src SH2 domain (IC50≈1 µM). Ac-Tyr(PO3H2)-Glu-Glu-Ile-Glu-OH TFA is an inhibitor for src SH3-SH2:phosphoprotein interactions .
rel-SB-612111 hydrochloride is a novel and potent human opiate receptor-like orphan receptor (ORL-1) antagonist with a highaffinity for hORL-1 (Ki=0.33 nM). rel-SB-612111 hydrochloride exhibits selectivity for μ-, κ- and δ-receptors with Ki values of 57.6 nM, 160.5 nM and 2109 nM, respecticely. rel-SB-612111 hydrochloride effectively antagonizes the pronociceptive action of Nociceptin (HY-P0183) in an acute pain model .
AM6538 is a long-acting, highaffinity and pseudo-irreversible cannabinoid (CB) antagonist. AM6538 is a structural analog of rimonabant. AM6538 can be effectively used to evaluate the apparent efficacy of cannabinoid full and partial agonists. AM6538 may be useful in future studies that require temporary reductions in cannabinoid receptor availability . AM-6538 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
CM398 is a highly selective, orally active sigma-2 receptor ligand (Ki=0.43 nM), with high sigma-1/sigma-2 selectivity rato (1000-fold). CM398 shows notable affinity for dopamine (Ki=32.90 nM) and serotonin transporters (Ki=244.2 nM). CM398 shows promising anti-inflammatory analgesic effects in the formalin model of inflammatory pain in mice .
Ozanimod (RPC-1063) hydrochloride, a sphingosine 1-phosphate (S1P) receptor modulator that binds with highaffinity selectively to S1P receptor subtypes 1 (S1P1) and 5 (S1P5). Ozanimod hydrochloride has modulate effect for hS1P1 and hS1P5 receptor with EC50s of 1.03 nM and 8.6 nM, respectively. Ozanimod hydrochloride can be used for the research of relapsing multiple sclerosis (MS) .
Toluidine Blue (Toluidine Blue O) purity 36% is an alkaline quinonimine dye (vivo dye) with highaffinity for acidic tissue components, staining nuclei blue and polysaccharides purple. Toluidine Blue purity 36% shows heterostaining properties for mast cells, mucins and chondrocytes. Toluidine Blue purity 36% can stain different components of plant tissues and cells in different colours. Toluidine Blue purity 36% is also used as a diagnostic aid to identify malignant lesions, such as cancer .
Tebentafusp (IMCgp100) is a bispecific fusion protein to target gp100 peptide-HLA-A*02:01 (a melanoma-associated antigen). Tebentafusp guides T cells to kill gp100-expressing tumor cells via a highaffinity T-cell receptor (TCR) binding domain and an anti-CD3 T-cell engaging domain. Tebentafusp leads to inflammatory cytokines and cytolytic proteins production, resulting in the direct lysis of tumour cells .
SB-216641A (SB-216641 hydrochloride) is a selective antagonist of 5-HT1B/D receptor. SB-216641A shows highaffinity and selectivity for h5-HT1B receptors over h5-HT1D receptors. SB-216641A inhibits the function of SKF-99101H .
Dicyclomine-d4 is the deuterium labeled Dicyclomine[1]. Dicyclomine (Dicycloverine) is a potent and orally active muscarinic cholinergic receptors antagonist. Dicyclomine (Dicycloverine) shows highaffinity for muscarinic M1 receptor subtype (Ki=5.1 nM) and M2 receptor subtype (Ki=54.6 nM) in brush-border membrane and basal plasma membranes, respectively[2]. Dicyclomine is an antispasmodic agent and relieves smooth muscle spasm of the gastrointestinal tract in vivo[3].
3′-Methoxyfurano[4″,5″:3,4]chalcone (compound 2) is a selective A2AAR antagonist (IC50=33.5 nM) with highaffinity. 3′-Methoxyfurano[4″,5″:3,4]chalcone is also a natural product obtained from the bark of Allium cepa L. 3′-Methoxyfurano[4″,5″:3,4]chalcone can promote T cell activation and can be used in cancer immunity research .
RIPK2-IN-5 (compound 14) is a highaffinity and excellent selectivity RIPK2 inhibitor with an IC50 value of 5.1nM. RIPK2-IN-5 has cellular anti-inflammatory effect and can reduce the secretion of MDP-induced TNF-α with a dose-dependent manner. RIPK2-IN-5 shows moderate stability in human liver microsome. RIPK2-IN-5 can be used for the research of immune diseases .
Clozapine (Standard) is the analytical standard of Clozapine. This product is intended for research and analytical applications. Clozapine (HF 1854) is an antipsychotic used for the research of schizophrenia. Clozapine has highaffinity for a number of neuroreceptors. Clozapine is a potent antagonist of dopamine D2 with a Ki of 75 nM. Clozapine inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor with Kis of 9.5 nM and 4 nM, respectively . Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM) .
Cendakimab (RPC4046; ABT 308; CC-93538) is a selective, humanized, recombinant monoclonal antibody against the IL-13 molecule. Cendakimab has a highaffinity and potency for both human wild-type and variant IL-13 and blocks binding of IL-13 to both IL-13Rα1 and IL-13Rα2 with IC50s of 352 pM and 631 pM by ELISA, respectively. Cendakimab recognizes both wild-type human IL-13 and the common polymorphic variant R110Q, with binding affinities of 52 and 50 pM, respectively. Cendakimab has the potential for IL-13-related allergic/inflammatory diseases (e.g., asthma and eosinophilic esophagitis) .
Aripiprazole (OPC-14597), an atypical antipsychotic, is a potent and high-affinitydopamine D2 receptor partial agonist. Aripiprazole is an inverse agonist at 5-HT2B and 5-HT2A receptors and displays partial agonist actions at 5-HT1A, 5-HT2C, D3, and D4 receptors. Aripiprazole can be used for the research of schizophrenia and COVID19 .
Cipralisant (GT-2331) is an orally active, low-toxicity, potent, selective, highaffinityhistamine H3 receptor full antagonist in vivo, and an agonist in vitro, with a pKi of 9.9 for histamine H3 receptor and a Ki of 0.47 nM for rat histamine H3 receptor. Cipralisant has the potential for attention-deficit hyperactivity disorder research . Cipralisant is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Propranolol-d7 is the deuterium labeled Propranolol. Propranolol is a nonselective β-adrenergic receptor (βAR) antagonist, has highaffinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively[1]. Propranolol inhibits [3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM[2]. Propranolol is used for the study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy[3].
FG 7142 (ZK 39106; LSU-65), a non-selectively benzodiazepine inverse agonist, has highaffinity for the α1 subunit-containing GABAA receptor (Ki=91 nM). FG 7142 (ZK 39106; LSU-65) also modulates GABA-induced chloride flux at GABAA receptors expressing the α1 subunit (EC50= 137 nM). FG 7142 (ZK 39106; LSU-65) can increase tyrosine hydroxylation and cause upregulation of β-adrenoceptors in mouse cerebral cortex .
Propranolol-d7 (hydrochloride) is a deuterium labeled Propranolol hydrochloride. Propranolol hydrochloride is a nonselective β-adrenergic receptor (βAR) antagonist, has highaffinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively[1]. Propranolol hydrochloride inhibits [3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM[2]. Propranolol hydrochloride is used for the study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy[3].
TIK-301 (PD-6735) is a chlorinated melatonin derivative and a potent, high-affinity and orally active melatonin MT1 and MT2 receptors agonist with Kis of 0.081 nM and 0.042 nM, respectively. TIK-301 is also a 5-HT2B/5-HT2C receptors antagonist with antidepressant action. TIK-301 has the potential for sleep disorders and other circadian rhythm disorders treatment .
A2ti-1 is a selective and high-affinityannexin A2/S100A10 heterotetramer (A2t) inhibitor with an IC50 of 24 μM . A2ti-1 specifically disrupts the protein-protein interaction (PPI) between A2 and S100A10. A2ti-1 prevents human papillomavirus type 16 (HPV16) infection .
NVS-CECR2-1, a non-BET family Bromodomain (BRD) inhibitor, is a potent and selective cat eye syndrome chromosome region, candidate 2 (CECR2) inhibitor. NVS-CECR2-1 binds to CECR2 BRD with highaffinity (IC50=47 nM; KD=80 nM). NVS-CECR2-1 exhibits cytotoxic activity and induces apoptosis against various cancer cells by targeting CECR2 as well as via CECR2-independent mechanism .
BET bromodomain inhibitor 1 is an orally active, selective bromodomain and extra-terminal (BET) bromodomain inhibitor with an IC50 of 2.6 nM for BRD4. BET bromodomain inhibitor 1 binds to BRD2(2), BRD3(2), BRD4(1), BRD4(2), and BRDT(2) with highaffinities (Kd values of 1.3 nM, 1.0 nM, 3.0 nM, 1.6 nM, 2.1 nM, respectively). bromodomain inhibitor 1 has anti-cancer activity .
Cipralisant (GT-2331) (maleate) is an orally active, low-toxicity, potent, selective, highaffinityhistamine H3 receptor full antagonist in vivo, and an agonist in vitro, with a pKi of 9.9 for histamine H3 receptor and a Ki of 0.47 nM for rat histamine H3 receptor. Cipralisant (maleate) has the potential for attention-deficit hyperactivity disorder research . Cipralisant (maleate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
LSD1/ER-IN-1 (compound 11g) is a potent ER and LSD1 inhibitor, with an IC50 of 1.55 μM (LSD1). LSD1/ER-IN-1 has highaffinity selectivity for ERα protein, with α/β ratio of 7.11. LSD1/ER-IN-1 shows good antiproliferative activity against MCF-7 breast cancer cells, with an IC50 of 8.79 μM .
Aripiprazole (OPC-14597) monohydrate, an atypical antipsychotic, is a potent and high-affinitydopamine D2 receptor partial agonist. Aripiprazole monohydrate is an inverse agonist at 5-HT2B and 5-HT2A receptors and displays partial agonist actions at 5-HT1A, 5-HT2C, D3, and D4 receptors. Aripiprazole monohydrate can be used for the research of schizophrenia and COVID19 .
SARS-CoV-2-IN-32 (compound 3g) is a COVID-19 inhibitor. SARS-CoV-2-IN-32 shows anti-proliferative activity against cancer cells. SARS-CoV-2-IN-32 exhibits comparatively high binding affinity (-8.8 Kcal/mole) to COVID-19 main protease (M pro) (PDB ID: 6LU7). SARS-CoV-2-IN-32 can be used in studies of cancer and COVID-19 .
TK-129 is an orally active, low-toxicity, potent KDM5B inhibitor (with highaffinity; IC50=44 nM). TK-129 exerts cardioprotective effects by inhibiting KDM5B and blocking the KDM5B-associated Wnt pathway. TK-129 reduces ang II-induced activation of cardiac fibroblasts in vitro and reduces isoprenaline-induced myocardial remodelling and fibrosis in vivo. TK-129 can be used in studies of cardiovascular disease .
DIBA-Cy5 is a fluorescent DIBA antagonist made up be DIBA-alkyne binding Cyanine5 fluorophores (Cy5) and polyethylene glycol (PEG) biomolecules. DIBA-Cy5 can serve as a fluorescent ligand, suitable for probe attachment through click chemistry. DIBA-Cy5 exerts a high binding affinity to type-2 mAChR (M2R) with the Kd value of 1.80 nM, can directly stain M2R receptors in the sinoatrial node of a mouse heart .
CB2R antagonist 3 is a selective antagonist of cannabinoid type 2 receptor (CB2R). CB2R antagonist 3 has highaffinity for human CB2R and specific selectivity for CB1R. CB2R antagonist 3 can be combined with CB65 (HY-110047), the activator of CB2R. CB2R antagonist 3 effectively up-regulates the expression of anti-inflammatory cytokines and down-regulates the expression of pro-inflammatory cytokines .
Cucurbit[7]uril is a cyclic organic molecule consisting of seven glycoluril units linked by methylene bridges. It has a rigid barrel-like structure with two identical inlets at both ends to selectively encapsulate guest molecules of appropriate size, shape, and polarity. Cucurbit[7]uril is known for its high binding affinity for a variety of organic and inorganic guests, including drugs, amino acids, peptides, and metal ions. This property makes them promising candidates for various applications in areas such as drug delivery, catalysis, and sensing.
(Rac)-BDA-366 (example 2) is the despinner of BDA-366 (HY-101083). BDA-366 is a potent Bcl-2 antagonist (Ki=3.3 nM), binding Bcl-2-BH4 domain with highaffinity and selectivity. BDA-366 induces conformational change in Bcl-2 that abrogates its antiapoptotic function, converting it from a survival molecule to a cell death inducer. BDA-366 suppresses growth of lung cancer cells .
PF-06372865 is an orally active, α2/α3/α5 subtype-selective GABAA positive allosteric modulator (PAM). PF-06372865 is a highaffinity ligand at GABAA receptors containing α1/α2/α3/α5 subunits (Kis of 2.9 nM, 21 nM, 134 nM for α2, α1 PAM, α2 PAM, respectively), with low affinity for α4/α6 subunits. PF-06372865 can across the blood-brain barrier (BBB). PF-06372865 has anxiolytic activity and has the potential for epilepsy .
Quetiapine hemifumarate is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine hemifumarate is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine hemifumarate has moderate to highaffinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects .
Quetiapine (ICI204636) is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine has moderate to highaffinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects .
Prucalopride is an orally active, selective and specific 5-HT 4 receptor agonist (highaffinity), with pKis of 8.6 and 8.1 for human 5-HT4a/4b receptors, respectively. Prucalopride improves intestinal motility by promoting regeneration of the intestinal nervous system in rats. Prucalopride also shows anticancer activity by blocking of the PI3K/AKT/mTor signaling pathway. Prucalopride can be used in studies of chronic constipation, pseudo-intestinal obstruction and cancer .
Ifenprodil tartrate is a typical noncompetitive NMDA receptor antagonist. Ifenprodil tartrate exerts highaffinity at NR1A/NR2B receptors (IC50=0.34 μM) over 400-fold than at NR1A/NR2A receptors (IC50=146 μM) . Ifenprodil tartrate inhibits GIRK (Kir3), reduces inward currents through the basal GIRK activity. Ifenprodil tartrate has the potential to be a cerebral vasodilator .
Metergoline is a serotonin (5-HT) receptor and dopamine receptors antagonist, with pKis of 8.64, 8.75 and 8.75 for 5-HT2A, 5-HT2B and 5-HT2C, respectively. Metergoline is a high-affinity ligand for the h5-HT7 receptor, with a Ki of 16 nM. Metergoline is also a reversible neural Na + channels inhibitor. Metergoline is commonly used for the research of seasonal affective disorder, prolactin hormone regulation .
Targapremir-210 (TGP-210) is a potent and selective miR-210 (miRNA-210, microRNA-210) inhibitor. Targapremir-210 inhibits pre-miR-210 processing with high binding affinity (Kd~200 nM) . Targapremir-210 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
Propranolol-d7 (ring-d7) is the deuterium labeled Propranolol hydrochloride. Propranolol hydrochloride is a nonselective β-adrenergic receptor (βAR) antagonist, has highaffinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively[1]. Propranolol hydrochloride inhibits [3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM[2]. Propranolol hydrochloride is used for study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy[3].
Pozanicline (ABT-089) selectively activate neuronal nicotinic acetylcholine receptor (nAChR) subtypes, is a novel cholinergic agent that is a partial agonist at α4β2* nAChRs (Ki=16 nM) and shows high selectivity for α6β2* and α4α5β2 nAChR subtypes, the binding affinity (Ki, rat) for Pozanicline to [ 3H] cytisine sites is 16.7 nM.
Pozanicline reverses nicotine withdrawal-induced cognitive deficits, may be an effective component of novel therapeutic strategies for nicotine addiction .
SCH79797 dihydrochloride is a highly potent, selective nonpeptide protease activated receptor 1 (PAR1) antagonist. SCH79797 dihydrochloride inhibits binding of a high-affinity thrombin receptor-activating peptide to PAR1 with an IC50 of 70 nM and a Ki of 35 nM. SCH79797 dihydrochloride inhibits thrombin-induced platelet aggregation with an IC50 of 3 μM. SCH79797 dihydrochloride has antiproliferative and pro-apoptotic effects, and limits myocardial ischemia/reperfusion injury in rat hearts. SCH79797 dihydrochloride also potently prevents PAR1 activation in vascular smooth muscle cells, endothelial cells, and astrocytes .
Brevetoxin-3 (PbTx-3) is a potent allosteric voltage-gated Na + channel activator and has multiple active centers (A-ring lactone, C-42 of R side chain) . Brevetoxin-3 (PbTx-3) has a highaffinity to site 5 of the voltage-sensitive Na + channels, inhibits the inactivation of Na + channels and prolongs the mean open time of these channels. Brevetoxin-3 (PbTx-3) repeated exposures can lead to prolonged airway hyperresponsiveness (AHR) and lung inflammation .
Lei-Dab7 TFA is a highaffinity, selective KCa2.2 (SK2) channel blocker (Kd=3.8 nM). Lei-Dab7 TFA exhibits >200-fold selectivity for KCa2.2 over KCa2.1, KCa2.3, KCa3.1, Kv and Kir2.1. Lei-Dab7 TFA increases theta-burst responses and increases LTP in rat hippocampal slices in vitro.
8-CPT-Cyclic AMP (8-CPT-cAMP) sodium is a selective activator of cyclic AMP-dependent protein kinase (PKA). 8-CPT-Cyclic AMP sodium is also a potent inhibitor of the cyclic GMP-specific phosphodiesterase (PDE VA) with an IC50 of 0.9 μM. 8-CPT-Cyclic AMP sodium also inhibits PDE III and PDE IV with IC50high affinity for Epac and is a potent Epac activator .
SCH79797 is a highly potent, selective nonpeptide protease activated receptor 1 (PAR1) antagonist. SCH79797 inhibits binding of a high-affinity thrombin receptor-activating peptide to PAR1 with an IC50 of 70 nM and a Ki of 35 nM. SCH79797 inhibits thrombin-induced platelet aggregation with an IC50 of 3 μM. SCH79797 has antiproliferative and pro-apoptotic effects, and limits myocardial ischemia/reperfusion injury in rat hearts. SCH79797 also potently prevents PAR1 activation in vascular smooth muscle cells, endothelial cells, and astrocytes .
Relugolix-d6 is deuterium labeled Relugolix. Relugolix (TAK-385) is a potent, orally active, nonpeptidic gonadotropin-releasing hormone (GnRH) antagonist. Relugolix possesses highaffinity and potent antagonistic activity for human receptor (binding IC50=0.33 nM) and monkey receptor (IC50=0.32 nM) compared with TAK-013 (HY-100209)[1]. Relugolix is used for the study of sex-hormone-dependent diseases, such as including endometriosis, uterine fibroids and prostate cancer et al[2].
Olanzapine (LY170053) is a selective, orally active monoaminergic antagonist with highaffinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptor (Ki=19 nM). Olanzapine is an atypical antipsychotic .
Vari Fluor 680-Streptavidin is a dye marker of Vari Fluor-streptavidin consisting of labeling streptavidin with a Vari Fluor series of fluorescent probes. Streptavidin is a high-affinity tetramer protein, each tetramer consisting of four identical streptavidin subunits. Streptavidin binds to biotin specifically via a reversible non-covalent effect. Streptavidin can achieve rapid and efficient detection of biotin markers, and is often used in immunofluorescence (IF), enzyme-linked immunosorbent assay (ELISA), immunohistochemical staining (IFH), in situ hybridization (ISH) and other experiments. Ex/Em=680 nm/701 nm.
Vari Fluor 647-Streptavidin is a dye marker of Vari Fluor-streptavidin consisting of labeling streptavidin with a Vari Fluor series of fluorescent probes. Streptavidin is a high-affinity tetramer protein, each tetramer consisting of four identical streptavidin subunits. Streptavidin binds to biotin specifically via a reversible non-covalent effect. Streptavidin can achieve rapid and efficient detection of biotin markers, and is often used in immunofluorescence (IF), enzyme-linked immunosorbent assay (ELISA), immunohistochemical staining (IFH), in situ hybridization (ISH) and other experiments. Ex/Em=650 nm/665 nm.
Vari Fluor 594-Streptavidin is a dye marker of Vari Fluor-streptavidin consisting of labeling streptavidin with a Vari Fluor series of fluorescent probes. Streptavidin is a high-affinity tetramer protein, each tetramer consisting of four identical streptavidin subunits. Streptavidin binds to biotin specifically via a reversible non-covalent effect. Streptavidin can achieve rapid and efficient detection of biotin markers, and is often used in immunofluorescence (IF), enzyme-linked immunosorbent assay (ELISA), immunohistochemical staining (IFH), in situ hybridization (ISH) and other experiments. Ex/Em=590 nm/617 nm.
Vari Fluor 555-Streptavidin is a dye marker of Vari Fluor-streptavidin consisting of labeling streptavidin with a Vari Fluor series of fluorescent probes. Streptavidin is a high-affinity tetramer protein, each tetramer consisting of four identical streptavidin subunits. Streptavidin binds to biotin specifically via a reversible non-covalent effect. Streptavidin can achieve rapid and efficient detection of biotin markers, and is often used in immunofluorescence (IF), enzyme-linked immunosorbent assay (ELISA), immunohistochemical staining (IFH), in situ hybridization (ISH) and other experiments. Ex/Em=555 nm/565 nm.
Vari Fluor 488-Streptavidin is a dye marker of Vari Fluor-streptavidin consisting of labeling streptavidin with a Vari Fluor series of fluorescent probes. Streptavidin is a high-affinity tetramer protein, each tetramer consisting of four identical streptavidin subunits. Streptavidin binds to biotin specifically via a reversible non-covalent effect. Streptavidin can achieve rapid and efficient detection of biotin markers, and is often used in immunofluorescence (IF), enzyme-linked immunosorbent assay (ELISA), immunohistochemical staining (IFH), in situ hybridization (ISH) and other experiments. Ex/Em=490 nm/515 nm.
Vari Fluor 405-Streptavidin is a dye marker of Vari Fluor-streptavidin consisting of labeling streptavidin with a Vari Fluor series of fluorescent probes. Streptavidin is a high-affinity tetramer protein, each tetramer consisting of four identical streptavidin subunits. Streptavidin binds to biotin specifically via a reversible non-covalent effect. Streptavidin can achieve rapid and efficient detection of biotin markers, and is often used in immunofluorescence (IF), enzyme-linked immunosorbent assay (ELISA), immunohistochemical staining (IFH), in situ hybridization (ISH) and other experiments. Ex/Em=405 nm/431 nm.
Izeltabart is a high-affinity humanized antibody targeting ADAM9. Izeltabart can be used as ADC Antibody for site-specific conjugation with Maytansinoid-based DM21-C (a Drug-Linker Conjugates for ADC), to synthesize IMGC936 (Antibody-Drug Conjugates (ADCs)) with strong anti-cancer activity. DM21-C is composed of Maytansinoid (microtubule inhibitor) and a stable tripeptide linker. IMGC936 exhibits cytotoxicity against ADAM9-positive human tumor cell lines and potent antitumor activity in xenograft tumor models .
Prucalopride hydrochloride is an orally active, selective and specific 5-HT4 receptor agonist (highaffinity), with pKis of 8.6 and 8.1 for human 5-HT4a/4b receptors, respectively. Prucalopride hydrochloride improves intestinal motility by promoting regeneration of the intestinal nervous system in rats. Prucalopride hydrochloride also shows anticancer activity by blocking of the PI3K/AKT/mTor signaling pathway. Prucalopride hydrochloride can be used in studies of chronic constipation, pseudo-intestinal obstruction and cancer .
Prucalopride succinate is an orally active, selective and specific 5-HT 4 receptor agonist (highaffinity), with pKis of 8.6 and 8.1 for human 5-HT4a/4b receptors, respectively. Prucalopride succinate improves intestinal motility by promoting regeneration of the intestinal nervous system in rats. Prucalopride succinate also shows anticancer activity by blocking of the PI3K/AKT/mTor signaling pathway. Prucalopride succinate can be used in studies of chronic constipation, pseudo-intestinal obstruction and cancer .
SB 242084 is a selective, competitive and high-affinity (pKi=9.0) 5-HT2C receptor antagonist (crosses the blood-brain barrier). SB 242084 increases basal activity of dopaminergic neurons in the ventral tegmental area (VTA) of the midbrain and dopamine release in the vomeronasal nucleus. SB 242084 also increases mitochondrial gene expression and oxidative metabolism via 5-HT2A receptor. SB 242084 has good research potential in the negative symptoms of anxiety, depression and schizophrenia, as well as in acute organ damage .
SB 242084 dihydrochloride is a selective, competitive and high-affinity (pKi=9.0) 5-HT2C receptor antagonist (crosses the blood-brain barrier). SB 242084 dihydrochloride increases basal activity of dopaminergic neurons in the ventral tegmental area (VTA) of the midbrain and dopamine release in the vomeronasal nucleus. SB 242084 dihydrochloride also increases mitochondrial gene expression and oxidative metabolism via 5-HT2A receptor. SB 242084 dihydrochloride has good research potential in the negative symptoms of anxiety, depression and schizophrenia, as well as in acute organ damage .
VUF10166 is a potent and high-affinity5-HT3 receptor antagonist, with Ki values of 0.04 nM (5-HT3A) and 22 nM (5-HT3AB). VUF10166 inhibits 5-HT-induced responses at 5-HT3A and 5-HT3AB receptors at nanomolar concentrations. At 5-HT3 receptor, VUF10166 at higher concentrations also acts as a partial agonist, with an EC50 of 5.2 μM .
Olanzapine-d3 is the deuterium labeled Olanzapine. Olanzapine is a selective, orally active monoaminergic antagonist with highaffinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptors (Ki=19 nM). Olanzapine is an atypical antipsychotic[1][2].
Aripiprazole (Standard) is the analytical standard of Aripiprazole. This product is intended for research and analytical applications. Aripiprazole (OPC-14597), an atypical antipsychotic, is a potent and high-affinitydopamine D2 receptor partial agonist. Aripiprazole is an inverse agonist at 5-HT2B and 5-HT2A receptors and displays partial agonist actions at 5-HT1A, 5-HT2C, D3, and D4 receptors. Aripiprazole can be used for the research of schizophrenia and COVID19 .
Quetiapine-d8 (fumarate) is the deuterium labeled Quetiapine. Quetiapine is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine has moderate to highaffinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects[1][2].
PS10 is a novel, potent and ATP-competitive pan-PDK inhibitor, inhibits all PDK isoforms with IC50 of 0.8 μM, 0.76 μM, 2.1 μM and 21.3 μM for PDK2, PDK4, PDK1, and PDK3, respectively. PS10 shows highaffinity for PDK2 (Kd= 239 nM) than for Hsp90 (Kd= 47 μM) . PS10 improves glucose tolerance, stimulates myocardial carbohydrate oxidation in diet-induced obesity. PS10 has the potential for the investigation of diabetic cardiomyopathy .PDK: pyruvate dehydrogenase kinase
Apelin-36(human) is an endogenous orphan G protein-coupled receptor APJ agonist, with an EC50 of 20 nM. Apelin-36(human) shows highaffinity to human APJ receptors expressed in HEK 293 cells (pIC50=8.61). Apelin-36 has been linked to two major types of biological activities: cardiovascular and metabolic. Apelin-36(human) inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ .
SARS-CoV-2-IN-34 (S-20-1) is a blood brain barrier penetrable pan-coronavirus (CoV) fusion inhibitor with broad-spectrum inhibitory activity. SARS-CoV-2-IN-34 effectively inhibits infection by pseudotyped and authentic SARS-CoV-2, and pseudotyped variants of concern (VOCs). SARS-CoV-2-IN-34 shows highaffinity to RBD in S1 and HR1 domain in S2 of SARS-CoV-2 S protein. SARS-CoV-2-IN-34 can be used for the research of infection .
AChE/BuChE/MAO-B-IN-1 (compound 19) is an inhibitor of human acetyl- (hAChE), butyrylcholinesterase (hBuChE) and monoamine oxidase-B (hMAO-B) with IC50s of 4.8 μM, 13.7 μM, and 1.11 μM, respectively. AChE/BuChE/MAO-B-IN-1 also exhibits highaffinity to both the σ1 and σ2 receptors with Ki values of 42.8 nM (human σ1 receptor) and 191 nM (rat σ2 receptor), respectively. AChE/BuChE/MAO-B-IN-1 can be used for Alzheimer’s disease research .
Cinrebafusp alfa (PRS 343) is a highaffinityCD137/HER2 bispecfic anticalin-based drug. Cinrebafusp alfa binds to recombinant human HER2 (Kd=0.3 nM) and human monomeric CD137 (4-1BB; Kd=5 nM). Cinrebafusp alfa facilitates T-cell costimulation by tumor-localized, HER2-dependent 4-1BB clustering and activation, further enhancing T-cell receptor-mediated activity and leading to tumor destruction. Cinrebafusp alfa has the potential for HER2+ solid tumors research .
TCO-GK-PEG4-NHS ester is an ADC Linker, and can be used for synthesis of [18F]AlF-NOTA-Tz-TCO-GK-2Rs15d. [18F]AlF-NOTA-Tz-TCO-GK-2Rs15d binds with highaffinity and immunoreactivity to HER2 . TCO-GK-PEG4-NHS ester is a click chemistry reagent, it contains a TCO group that can undergo an inverse electron demand Diels-Alder reaction (iEDDA) with molecules containing Tetrazine groups.
Olanzapine (Standard) is the analytical standard of Olanzapine. This product is intended for research and analytical applications. Olanzapine (LY170053) is a selective, orally active monoaminergic antagonist with highaffinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptor (Ki=19 nM). Olanzapine is an atypical antipsychotic .
Silodosin (KAD 3213; KMD 3213) is a potent, selective and orally active α1A-adrenergic receptor (α1A-AR) blocker. Silodosin exhibits highaffinity for α1A-AR (Ki=0.036 nM), over 162-fold and 50-fold than for α1B-AR and α1D-AR with Ki values of 21 nM and 2.0 nM, respectively. Silodosin is an effective and well-tolerated agent, it can be used for the investigation of LUTS/BPH .
Quetiapine-d8 (hemifumarate) is the deuterium labeled Quetiapine hemifumarate. Quetiapine hemifumarate is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine hemifumarate is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine hemifumarate has moderate to highaffinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects[1].
THIQ is the first selective agonist of the melanocortin-4 receptor (MC4R), with highaffinity and potency for hMC4R (IC50=1.2 nM, EC50=2.1 nM) and rMC4R (IC50=0.6 nM, EC50=2.9 nM). THIQ maintains low potency at MC1R, MC3R and MC5R. THIQ plays a role in eliciting erectile activity in rodents. THIQ acts as a pharmacoperone of the MC4R rescuing the cell surface expression and signaling of some intracellularly retained MC4R mutants .
Apelin-36(human) TFA is an endogenous orphan G protein-coupled receptor APJ agonist, with an EC50 of 20 nM. Apelin-36(human) TFA shows highaffinity to human APJ receptors expressed in HEK 293 cells (pIC550=8.61). Apelin-36(human) TFA has been linked to two major types of biological activities: cardiovascular and metabolic. Apelin-36(human) TFA inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ .
Quetiapine (hemifumarate)-d8 is the deuterium labeled Quetiapine hemifumarate[1]. Quetiapine hemifumarate is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine hemifumarate is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine hemifumarate has moderate to highaffinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects[2].
Quetiapine (hemifumarate) (Standard) is the analytical standard of Quetiapine (hemifumarate). This product is intended for research and analytical applications. Quetiapine hemifumarate is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine hemifumarate is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine hemifumarate has moderate to highaffinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects .
YO-PRO-1 (Oxazole yellow) is a carbocyanine monomer and DNA green fluorescent dye that is not permeable to normal animal cell membranes but is permeable to the cell membranes of apoptotic and necrotic cells. YO-PRO-1 is commonly used for the detection of apoptosis and necrosis. YO-PRO-1 has a highaffinity for DNA and is essentially non-fluorescent when not bound to DNA. When apoptosis occurs, the permeability of the cell membrane changes. YO-PRO-1 can enter apoptotic cells and bind to DNA and emit bright green fluorescence. Therefore, YO-PRO-1 is often used together with propidium iodide (PI) to analyze and identify apoptotic and necrotic cells.
Silodosin-d4 is the deuterium labeled Silodosin. Silodosin (KAD 3213) is a potent, selective and orally active α1A-adrenergic receptor (α1A-AR) blocker. Silodosin exhibits highaffinity for α1A-AR (Ki=0.036 nM), over 162-fold and 50-fold than for α1B-AR and α1D-AR with Ki values of 21 nM and 2.0 nM, respectively. Silodosin is an effective and well-tolerated agent, it can be used for the investigation of LUTS/BPH[1][3].
ELA-32(human) TFA is a potent, highaffinity apelin receptor agonist (IC50=0.27 nM; Kd=0.51 nM). ELA-32(human) TFA exhibits no binding GPR15 and GPR25. ELA-32(human) TFA activates the PI3K/AKT pathway and promotes self-renewal of hESCs via cell-cycle progression and protein translation. ELA-32(human) TFA also potentiates the TGFβ pathway, priming hESCs toward the endoderm lineage. ELA-32(human) TFA stimulates angiogenesis in HUVEC cells.
Ethidium homodimer (EthD-1) is a high-affinity fluorescent nucleic acid dye commonly used to stain mammals, bacteria, yeast, and fungi. Ethidium homodimer binds to DNA or RNA, enhancing fluorescence more than 30 times. The Ethidium homodimer has a strong positive charge, so it cannot cross cell membranes and stain living cells; But the Ethidium homodimer can cross the disordered region of the dead cell membrane to reach the nucleus and embed the DNA double strand to produce red fluorescence. Therefore, Ethidium homodimer is a relatively sensitive nucleic acid stain that can accurately detect nucleic acids in solution or in decomposing cells. Ethidium homodimer binds DNA, Ex/Em=528/617 nm .
SFNGGP-NH2 is a biological active peptide. (PAR-3 is a high-affinity thrombin receptor. PAR-3 mRNA is expressed in the cutaneous mast cells of humans. Protease-Activated Receptors (PARs) have been studied for their roles in itch and their itch-associated response through histamine-dependent/independent pathways have been reported. PAR-3 has been shown not to induce itching alone but possibly in conjunction with PAR-4. Co-expression of PAR-3 and PAR-4 enhances thrombin action suggesting that PAR-3 alone does not mediate transmembrane signaling but instead functions as a cofactor to activate PAR-4.)
A-366 is a potent, highly selective, peptide-competitive histone methyltransferase G9a inhibitor with IC50s of 3.3 and 38 nM for G9a and GLP (EHMT1), respectively. A-366 shows >1000-fold selectivity over 21 other methyltransferases. A-366 is also a potent, nanomolar inhibitor of the Spindlin1-H3K4me3-interaction (IC50=182.6 nM). A-366 displays highaffinity at human histamine H3 receptor (Ki=17 nM) and shows subtype selectivity among subsets of the histaminergic and dopaminergic receptor families .
ERRα antagonist-1 (Compound A) is a selective and highaffinityestrogen-related receptor α (ERRα) antagonist. ERRα antagonist-1 inhibits interaction of ERRα with Proliferator-activated Receptor γ Coactivator-1α (PGC-1α) and PGC-1β, the IC50 values are 170 nM and 180 nM, respectively. ERRα antagonist-1 does not inhibit the interaction of either ERRβ or ERRγ with PGC-1α and PGC-1β coactivator, and also does not inhibit interaction of ERα or ERβ with PGC-1α or SRC-1 .
CYM50308 (ML248) is a potent, selective and highaffinitysphingosine-1-phosphate receptor 4 (S1P4-R) agonist with an EC50 of 56 nM. CYM50308 displays 37-fold more selective for S1P4-R than S1P5-R. CYM50308 has no activity at S1P1-R, S1P2-R and S1P3-R subtypes at concentrations up to 25 μM .
L6H21, a Chalcone (HY-121054) derivative, is an orally active, potent and specific myeloid differentiation 2 (MD-2) inhibitor. L6H21 directly binds to MD-2 protein with a highaffinity and low KD value of 33.3 μM, blocking the formation of the LPS-TLR4/MD-2 complex. L6H21 inhibits LPS-induced expression of TNF-α and IL-6 in RAW264.7 macrophages, with IC50 values of 6.58 and 8.59 μM, respectively. L6H21 can be used for alcoholic liver disease, metabolic disturbance and neuroinflammation research .
HIV-1 inhibitor-51, a non-nucleoside reverse transcriptase inhibitor (NNRTI), exhibits outstanding antiviral activity against WT HIV-1 (IIIB) and a panel of mutant strains. HIV-1 inhibitor-51 has high binding affinity (KD=2.50 μM) and inhibitory activity (IC50=0.03 μM) to WT HIV-1 RT. HIV-1 inhibitor-51 has EC50s of 2.22-53.3 nM for mutant strains (L100I, K103N, Y181C, Y188L, E138K, F227L + V106A, RES056) .
MC-GGFG-AM-(10Me-11F-Camptothecin) is a linker-payload conjugate used to synthesize ZW251. ZW251 an antibody-drug conjugate (ADC) targeting human GPC3. ZW251 consists of a humanized IgG1 antibody conjugated to a novel camptothecin-based topoisomerase 1 inhibitor, ZD06519, via a linker. The linker is the maleimide anchor and a glycyl glycyl phenylalanyl glycine (GGFG)-aminomethyl (AM) cleavable linker. ZW251 has highaffinity with human and cynomolgus monkey GPC3. ZW251 displays rapid internalization in GPC3-expressing HCC cell lines, and bystander-mediated killing of GPC3 negative cancer cells .
AVN-101 hydrochloride is a potent, brain-penetrant and orally active 5-HT7 receptor antagonist (Ki of 153 pM), with slightly lesser potency toward 5-HT6, 5-HT2A, and 5HT-2C receptors (Ki values of 2.04 nM, 1.56 nM, and 1.17 nM, respectively). AVN-101 hydrochloride also exhibits a rather highaffinity toward histamine H1 (Ki of 0.58 nM) and adrenergic α2A, α2B, and α2C (Ki= 0.41-3.6 nM) receptors. AVN-101 hydrochloride can be studied in such diseases as general anxiety disorders, depression, schizophrenia, and multiple sclerosis .
Frovatriptan succinate hydrate ((R)-Frovatriptan succinate hydrate) is a potent, highaffinity, selective and orally active 5-HT1B (pK50 of 8.2) and 5-HT1D receptor agonist. Frovatriptan succinate hydrate exhibits >10-fold selectivity for 5-HT1B and 5-HT1D over 5-HT1A, 5-HT1F, and 5-HT7 and >1000-fold selectivity over other 5-HT, dopamine, histamine H1, and α1-adrenoceptor. Frovatriptan succinate hydrate has the potential for migraine research .
PF-04995274 is a potent, high-affinity, orally active and partial serotonin 4 receptor (5-HT4R) agonist. PF-04995274 has an EC50 range of 0.26-0.47 nM for human 5-HT4A/4B/4D/4E (Ki range of 0.15-0.46 nM), and has an EC50 range of 0.59-0.65 nM for rat 5-HT4S/4L/4E (Ki of 0.30 nM for rat 5-HT4S). PF-04995274 is brain penetrant and can be used for cognitive disorders associated with Alzheimer's disease .
Frovatriptan succinate ((R)-Frovatriptan succinate) is a potent, highaffinity, selective and orally active 5-HT1B (pK50 of 8.2) and 5-HT1D receptor agonist. Frovatriptan succinate exhibits >10-fold selectivity for 5-HT1B and 5-HT1D over 5-HT1A, 5-HT1F, and 5-HT7 and >1000-fold selectivity over other 5-HT, dopamine, histamine H1, and α1-adrenoceptor. Frovatriptan succinate has the potential for migraine research .
Lds-751 is a nucleic acid stain that mainly detects DNA. Lds-751 is a nucleic acid stain that mainly detects DNA. Lds-751 has a highaffinity for DNA and fluorescence is enhanced after binding, but the maximum emission wavelength is 670nm. Lds-751 and Thiazole orange can be used for the differentiation of red blood cells, platelets, reticulocytes, and nucleated cells and can be stimulated at 488nm. Studies have shown that LDS-751 binds almost exclusively to mitochondria when incubated with nucleated living cells. After nucleated Acridine Orange (HY-101879) staining and LDS-751 treatment of cells, confocal microscopy revealed almost no co-location of the cells. Staining with Rhodamine 123 (HY-D0816), a dye known to bind polarized mitochondria, was almost identical to the pattern observed with LDS-751 .
Frovatriptan-d3 (succinate) is deuterium labeled Frovatriptan (succinate). Frovatriptan succinate ((R)-Frovatriptan succinate) is a potent, highaffinity, selective and orally active 5-HT1B (pK50 of 8.2) and 5-HT1D receptor agonist. Frovatriptan succinate exhibits >10-fold selectivity for 5-HT1B and 5-HT1D over 5-HT1A, 5-HT1F, and 5-HT7 and >1000-fold selectivity over other 5-HT, dopamine, histamine H1, and α1-adrenoceptor. Frovatriptan succinate has the potential for migraine research[1][2].
Macrocycles, molecules containing 12-membered or larger rings, are receiving increased attention in small-molecule drug discovery. The reasons are several, including providing access to novel chemical space, challenging new protein targets, showing favorable ADME- and PK-properties. Macrocycles have demonstrated repeated success when addressing targets that have proved to be highly challenging for standard small-molecule drug discovery, especially in modulating macromolecular processes such as protein–protein interactions (PPI). Otherwise, the size and complexity of macrocyclic compounds make possible to ensure numerous and spatially distributed binding interactions, thereby increasing both binding affinity and selectivity.
MCE offers a unique collection of 364 macrocyclic compounds which can be used for drug discovery for high throughput screening (HTS) and high content screening (HCS). MCE Macrocyclic Compound Library is a useful tool for discovering new drugs, especially for “undruggable” targets and protein–protein interactions.
Peptidomimetics are compounds whose essential elements (pharmacophore) mimic a natural peptide or protein in 3D space and which retain the ability to interact with the biological target and produce the same biological effect. Peptidomimetics are designed to circumvent some of the problems associated with a natural peptide: e.g. stability against proteolysis (duration of activity) and poor bioavailability. Certain other properties, such as receptor selectivity or potency, often can be substantially improved. The design and synthesis of peptidomimetics are most important because of the dominant position peptide and protein-protein interactions play in molecular recognition and signaling, especially in living systems. Hence mimics have great potential in drug discovery.
MCE Peptidomimetic Library contains 376 compounds including peptoid, α-helix mimetics, β-turn/sheets mimetics, etc. This library is an indispensable tool of structure-activity relationships in drug discovery.
DCDAPH (Compound 2c) is a novel smart NIRF probe for detection of β-amyloid (Aβ) plaques (λex/λem=597/665 nm in PBS). DCDAPH shows highaffinity for Aβ aggregates (Ki=37 nM, Kd=27 nM). DCDAPH shows good blood brain barrier permeation and can meet most of the requirements for the detection of Aβ plaques both in vitro and in vivo .
Halo tag TMR is a fluorescent dye composed of Halo tag ligand molecules and TMR. Halo tag can rapidly form stable covalent binding with Halo protein with high specificity and highaffinity .
Fluo-3FF pentapotassium is a cell-permeable acetoxy-methyl ester of Fluo-3FF, a fluorescent calcium indicator. Fluo-3FF is a di-fluorinated analog of Fluo-3 with a 100-fold lower affinity than Fluo-3 for calcium (Kds = 42 and 0.4 碌M, respectively). For its low affinity, Fluo-3FF is used for studying compartments with high concentrations of calcium, such as endoplasmic reticulum, where highaffinity dyes will be insensitive to luminal fluctuations.
Fura-FF pentapotassium is a low-affinity fluorescent dye for calcium (Ex/Em: 365/514 nm in the absence of calcium; 339/507 nm in the presence of a high calcium concentration) .
Dansylcadaverine (Monodansyl cadaverine) is an autofluorescent compound used for the labeling of autophagic vacuoles. Dansylcadaverine, a highaffinity substrate of transglutaminases, can block the receptor-mediated endocytosis of many ligands .
Fluo-3 AM is a fluorecent Ca 2+ chelator, with highaffinity for calcium. Fluo-3 AM can specifically identify intracellular calcium ions, with high sensitivity, low cytotoxicity, increased AM acetylmethyl ester can enter the cell well, after being sheared by the intracellular esterase stay in the cell to bind to calcium ions, produce strong fluorescence .
QM-FN-SO3 is a BBB-penetrable near-infrared (NIR) aggregation-induced emission (AIE)-active probe for Aβ plaques. QM-FN-SO3 can be used for in vivo detection of Aβ plaques. QM-FN-SO3 has ultra-high S/N ratio, binding affinity, and high-performance NIR emission .
Quin-2AM is a fluorecent Ca 2+ chelator, with highaffinity for calcium. Quin-2AM can specifically identify intracellular calcium ions, with high sensitivity, low cytotoxicity, increased AM acetylmethyl ester can enter the cell well, after being sheared by the intracellular esterase stay in the cell to bind to calcium ions, produce strong fluorescence .
Mag-Fluo-4 AM is a fluorecent Ca 2+ chelator, with highaffinity for calcium. Mag-Fluo-4 AM can specifically identify intracellular calcium ions, with high sensitivity, low cytotoxicity, increased AM acetylmethyl ester can enter the cell well, after being sheared by the intracellular esterase stay in the cell to bind to calcium ions, produce strong fluorescence .
Fluo-4FF AM is a cell-permeant fluorescent calcium indicator. Fluo-4FF is an analog of Fluo-4 with a lower affinity for calcium, which is suitable for investigation of relatively high level of intracellular calcium.
QM-FN-SO3 ammonium is a BBB-penetrable near-infrared (NIR) aggregation-induced emission (AIE)-active probe for Aβ plaques. QM-FN-SO3 ammonium can be used for in vivo detection of Aβ plaques. QM-FN-SO3 ammonium has ultra-high S/N ratio, binding affinity, and high-performance NIR emission .
Phenosafranine is a phenazine dye. Phenosafranine has high binding affinity to triplex RNA compared to the parent duplex form, binds through intercalation to both forms of RNA. Phenosafranine can be used for staining plant cells, determination of hemoglobin, dopamine, serotonin and so on .
Fura-FF AM is a cell-permeable acetoxymethyl ester of fura-FF, a dluorescent calcium indicator. Fura-FF AM is hydrolyzed by intracellular esterases to release fura-FF in cells. Fura-FF is a difluorinated derivative of the calcium indicator fura-2. Compared to fura-2, fura-FF has a low affinity for calcium and is suitable for studying compartments with high concentrations of calcium.
Coppersensor-1 (CS1) is a membrane-permeable fluorescent dye. Coppersensor-1 has a picomolar affinity for Cu + with high selectivity over competing cellular metalions. Coppersensor-1 as a probe, can selective and sensitive detection of copper(I) ions (Cu +) in biological samples, including live cells. Coppersensor-1 can be used for the research of imaging of severe diseases such as cancer, cardiovascular disorders and neurogenerative diseases .
Rhod-2 is a high-affinity visible light excitation wavelength Ca 2+ fluorescent probe, Rhod-2, AM is an acetyl methyl ester derivative of Rhod-2, which has cell membrane permeability and can easily enter cells with simple culture. Once it enters the cell, it is sheared by its lactesterase to produce Rhod-2 without membrane permeability, which remains in the cell to perform the corresponding physiological functions. Maximum excitation/emission wavelength: 549/578 nm .
Toluidine Blue (Toluidine Blue O) purity 36% is an alkaline quinonimine dye (vivo dye) with highaffinity for acidic tissue components, staining nuclei blue and polysaccharides purple. Toluidine Blue purity 36% shows heterostaining properties for mast cells, mucins and chondrocytes. Toluidine Blue purity 36% can stain different components of plant tissues and cells in different colours. Toluidine Blue purity 36% is also used as a diagnostic aid to identify malignant lesions, such as cancer .
DIBA-Cy5 is a fluorescent DIBA antagonist made up be DIBA-alkyne binding Cyanine5 fluorophores (Cy5) and polyethylene glycol (PEG) biomolecules. DIBA-Cy5 can serve as a fluorescent ligand, suitable for probe attachment through click chemistry. DIBA-Cy5 exerts a high binding affinity to type-2 mAChR (M2R) with the Kd value of 1.80 nM, can directly stain M2R receptors in the sinoatrial node of a mouse heart .
Vari Fluor 680-Streptavidin is a dye marker of Vari Fluor-streptavidin consisting of labeling streptavidin with a Vari Fluor series of fluorescent probes. Streptavidin is a high-affinity tetramer protein, each tetramer consisting of four identical streptavidin subunits. Streptavidin binds to biotin specifically via a reversible non-covalent effect. Streptavidin can achieve rapid and efficient detection of biotin markers, and is often used in immunofluorescence (IF), enzyme-linked immunosorbent assay (ELISA), immunohistochemical staining (IFH), in situ hybridization (ISH) and other experiments. Ex/Em=680 nm/701 nm.
Vari Fluor 647-Streptavidin is a dye marker of Vari Fluor-streptavidin consisting of labeling streptavidin with a Vari Fluor series of fluorescent probes. Streptavidin is a high-affinity tetramer protein, each tetramer consisting of four identical streptavidin subunits. Streptavidin binds to biotin specifically via a reversible non-covalent effect. Streptavidin can achieve rapid and efficient detection of biotin markers, and is often used in immunofluorescence (IF), enzyme-linked immunosorbent assay (ELISA), immunohistochemical staining (IFH), in situ hybridization (ISH) and other experiments. Ex/Em=650 nm/665 nm.
Vari Fluor 594-Streptavidin is a dye marker of Vari Fluor-streptavidin consisting of labeling streptavidin with a Vari Fluor series of fluorescent probes. Streptavidin is a high-affinity tetramer protein, each tetramer consisting of four identical streptavidin subunits. Streptavidin binds to biotin specifically via a reversible non-covalent effect. Streptavidin can achieve rapid and efficient detection of biotin markers, and is often used in immunofluorescence (IF), enzyme-linked immunosorbent assay (ELISA), immunohistochemical staining (IFH), in situ hybridization (ISH) and other experiments. Ex/Em=590 nm/617 nm.
Vari Fluor 555-Streptavidin is a dye marker of Vari Fluor-streptavidin consisting of labeling streptavidin with a Vari Fluor series of fluorescent probes. Streptavidin is a high-affinity tetramer protein, each tetramer consisting of four identical streptavidin subunits. Streptavidin binds to biotin specifically via a reversible non-covalent effect. Streptavidin can achieve rapid and efficient detection of biotin markers, and is often used in immunofluorescence (IF), enzyme-linked immunosorbent assay (ELISA), immunohistochemical staining (IFH), in situ hybridization (ISH) and other experiments. Ex/Em=555 nm/565 nm.
Vari Fluor 488-Streptavidin is a dye marker of Vari Fluor-streptavidin consisting of labeling streptavidin with a Vari Fluor series of fluorescent probes. Streptavidin is a high-affinity tetramer protein, each tetramer consisting of four identical streptavidin subunits. Streptavidin binds to biotin specifically via a reversible non-covalent effect. Streptavidin can achieve rapid and efficient detection of biotin markers, and is often used in immunofluorescence (IF), enzyme-linked immunosorbent assay (ELISA), immunohistochemical staining (IFH), in situ hybridization (ISH) and other experiments. Ex/Em=490 nm/515 nm.
Vari Fluor 405-Streptavidin is a dye marker of Vari Fluor-streptavidin consisting of labeling streptavidin with a Vari Fluor series of fluorescent probes. Streptavidin is a high-affinity tetramer protein, each tetramer consisting of four identical streptavidin subunits. Streptavidin binds to biotin specifically via a reversible non-covalent effect. Streptavidin can achieve rapid and efficient detection of biotin markers, and is often used in immunofluorescence (IF), enzyme-linked immunosorbent assay (ELISA), immunohistochemical staining (IFH), in situ hybridization (ISH) and other experiments. Ex/Em=405 nm/431 nm.
YO-PRO-1 (Oxazole yellow) is a carbocyanine monomer and DNA green fluorescent dye that is not permeable to normal animal cell membranes but is permeable to the cell membranes of apoptotic and necrotic cells. YO-PRO-1 is commonly used for the detection of apoptosis and necrosis. YO-PRO-1 has a highaffinity for DNA and is essentially non-fluorescent when not bound to DNA. When apoptosis occurs, the permeability of the cell membrane changes. YO-PRO-1 can enter apoptotic cells and bind to DNA and emit bright green fluorescence. Therefore, YO-PRO-1 is often used together with propidium iodide (PI) to analyze and identify apoptotic and necrotic cells.
Ethidium homodimer (EthD-1) is a high-affinity fluorescent nucleic acid dye commonly used to stain mammals, bacteria, yeast, and fungi. Ethidium homodimer binds to DNA or RNA, enhancing fluorescence more than 30 times. The Ethidium homodimer has a strong positive charge, so it cannot cross cell membranes and stain living cells; But the Ethidium homodimer can cross the disordered region of the dead cell membrane to reach the nucleus and embed the DNA double strand to produce red fluorescence. Therefore, Ethidium homodimer is a relatively sensitive nucleic acid stain that can accurately detect nucleic acids in solution or in decomposing cells. Ethidium homodimer binds DNA, Ex/Em=528/617 nm .
Lds-751 is a nucleic acid stain that mainly detects DNA. Lds-751 is a nucleic acid stain that mainly detects DNA. Lds-751 has a highaffinity for DNA and fluorescence is enhanced after binding, but the maximum emission wavelength is 670nm. Lds-751 and Thiazole orange can be used for the differentiation of red blood cells, platelets, reticulocytes, and nucleated cells and can be stimulated at 488nm. Studies have shown that LDS-751 binds almost exclusively to mitochondria when incubated with nucleated living cells. After nucleated Acridine Orange (HY-101879) staining and LDS-751 treatment of cells, confocal microscopy revealed almost no co-location of the cells. Staining with Rhodamine 123 (HY-D0816), a dye known to bind polarized mitochondria, was almost identical to the pattern observed with LDS-751 .
Dmt-2'fluoro-da(bz) amidite, an uniformly modified 2'-deoxy-2'-fluoro phosphorothioate oligonucleotide, is a nuclease-resistant antisense compound with highaffinity and specificity for RNA targets. Dmt-2'fluoro-da(bz) amidite is also an intermediate for 5’-DMT-3’-phosphoramidite synthesis .
Evans Blue (Direct Blue 53) is a potent inhibitor of L-glutamate uptake via the membrane bound excitatory amino acid transporter (EAAT). Evans Blue is a L-glutamate and kainate receptor-mediated currents inhibitor. Evans Blue has a strong affinity towards serum albumin, making it a high molecular weight protein tracer. Evans Blue is also used to study BBB (blood-brain barrier) permeability .
Cucurbit[7]uril is a cyclic organic molecule consisting of seven glycoluril units linked by methylene bridges. It has a rigid barrel-like structure with two identical inlets at both ends to selectively encapsulate guest molecules of appropriate size, shape, and polarity. Cucurbit[7]uril is known for its high binding affinity for a variety of organic and inorganic guests, including drugs, amino acids, peptides, and metal ions. This property makes them promising candidates for various applications in areas such as drug delivery, catalysis, and sensing.
TTHA is a complexonate with highaffinity towards light rare earth elements (LREE), especially for La 3+ in ternary mixtures and Y 3+ in quinary mixtures .
ZnAF-2, 6-iso- is a cell-impermeable compound that acts as a high-affinity Zn2 -specific fluorescent probe (Kd = 2.7 nM). It exhibits low basal fluorescence with an approximately 51-fold increase in fluorescence intensity upon stoichiometric (1:1) binding to Zn2 . Little affinity for Ca2 , Mg2 , Na or K .
Endomorphin 2, a highaffinity, highly selective agonist of the μ-opioid receptor, displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM.
Acetalin-3 (Ac-RFMWMT-NH2), a hexapeptide, is a μ opioid receptor antagonist with highaffinity for μ and κ3 opioid receptor, weak affinity for κ1 receptors and no affinity for κ2 receptors .
Acetalin-1 (Ac-RFMWMK-NH2), a hexapeptide, is a μ opioid receptor antagonist with highaffinity for μ and κ3 opioid receptor, weak affinity for κ1 receptors and no affinity for κ2 receptors .
Endomorphin 2 TFA, a highaffinity, highly selective agonist of the μ-opioid receptor, displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM .
Neurotensin, a gut tridecapeptide, acts as a potent cellular mitogen for various colorectal and pancreatic cancers which possess high-affinityneurotensin receptors (NTR).
Endomorphin 1, a highaffinity, highly selective agonist of the μ-opioid receptor (Ki: 1.11 nM), displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM. Endomorphin 1 has antinociceptive properties .
Endomorphin 1 acetate, a highaffinity, highly selective agonist of the μ-opioid receptor (Ki: 1.11 nM), displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM. Endomorphin 1 acetate has antinociceptive properties .
Galanin-Like Peptide (porcine) is a 60 amino acid neuropeptide that was first isolated from the porcine hypothalamus. Galanin-Like Peptide (porcine) has a highaffinity for the GALR2 receptor (IC50 of 0.24 nM) and a lower affinity for the GALR1 receptor (IC50 of 4.3 nM) .
apoB (4372-4392) is a potent lipoprotein(a) assembly inhibitor, with an IC50 of 40 μM. apoB (4372-4392) can noncovalently bind to apolipoprotein(a) with highaffinity .
LGLLLRHLRHHSNLLANI (B18) is an 18 amino acid peptide. LGLLLRHLRHHSNLLANI derives from the membrane-associated protein binding. LGLLLRHLRHHSNLLANI shows a highaffinity for Cu(2+) ions .
Amylin, amide, rat is a potent and highaffinity ligand of Amylin receptor AMY1 and AMY3 receptors and variably of AMY2 receptors; binding studies are generally used for the latter receptor.
Prolactin Releasing Peptide (12-31), human is a fragment of the prolactin releasing peptide (PrRP). Prolactin Releasing Peptide (1-31), human is a highaffinityGPR10 ligand that cause the release of the prolactin.
Urocortin III (mouse) (free acid) is a selective CRF2 receptor agonist (with highaffinity for the CRF2 receptor). Urocortin III (mouse) (free acid) significantly inhibits gastric emptying without modifying colonic transit .
DOTA-NOC (DOTA-Nal3-octreotide) is a high-affinity ligand of somatostatin receptor subtypes 2, 3 and 5. DOTA-NOC can be used for labeling with various radiometals, and development of radiopeptide imaging .
CCZ01048 TFA, a α-MSH analogue, exhibits high binding affinity to melanocortin 1 receptor (MC1R) with a Ki of 0.31 nM. CCZ01048 TFA shows rapid internalization into B16F10 melanoma cells and high in vivo stability. CCZ01048 TFA is a promising candidate for PET imaging of malignant melanoma .
α-Conotoxin SIA is a selective nicotinic acetylcholine receptor (nAChR) antagonist with highaffinity for the muscle nAChR. α-Conotoxin SIA preferentially targets the α/δ interface of the muscle nAChR in mouse muscle. In contrast, for Torpedo nAChR, α-Conotoxin SIA has a much higher affinity for the α/γ than for the α/δ interface .
LDV-FITC, a fluorescent peptide, is a FITC-conjugated LDV peptide (HY-P2267). LDV-FITC binds to the α4β1 integrin with highaffinity (Kd: 0.3 nM and 12 nM for binding to U937 cells in the presence and absence of Mn 2+ respectively). LDV-FITC can be used to detect α4β1 integrin affinity .
CCZ01048, a α-melanocyte-stimulating hormone (α-MSH) analogue, exhibits high binding affinity to melanocortin 1 receptor (MC1R) with a Ki of 0.31 nM. CCZ01048 shows rapid internalization into B16F10 melanoma cells and high in vivo stability. CCZ01048 is a promising candidate for PET imaging of malignant melanoma .
Pancreatic Polypeptide, bovine, a 36-amino acid, straight chain polypeptide derived primarily from the pancreas, inhibits secretin- and cholecystokinin-stimulated pancreatic secretion; Pancreatic Polypeptide, bovine acts as an agonist of NPY receptor, with highaffinity at NPYR4.
p5 Ligand for Dnak and DnaJ is a nonapeptide, which corresponds to the main binding site for the 23-residue part of the presequence of mitochondrial aspartate aminotransferase. p5 Ligand for Dnak and DnaJ is a high-affinity ligand for DnaK and DnaJ .
β-Endorphin, equine TFA is an endogenous opioid peptide, which binds at highaffinity to both μ/δ opioid receptors. β-Endorphin, equine TFA has analgesic properties .
Endotoxin inhibitor a synthetic peptide that binds lipid A with highaffinity, thereby detoxifying LPS (HY-D1056) and preventing LPS-induced cytokine release in vivo. Endotoxin inhibitor inhibits the febrile response to LPS with very low toxicity and lethality .
α-Conotoxin GI has highaffinity for nAChR.α-Conotoxin GI is a short peptide toxin that can be isolated from the venom of Conus geographus.α-Conotoxin GI has the similar activity with neuromuscular blocking agent .
S961 is an high-affinity and selective insulin receptor (IR) antagonist with IC50s of 0.048, 0.027, and 630 nM for HIR-A, HIR-B, and human insulin-like growth factor I receptor (HIGF-IR) in SPA-assay, respectively .
SNX-482, a peptidyl toxin of the spider Hysterocrates gigas, is a potent, highaffinity, selective and voltage-dependent R-type CaV2.3 channel blocker with an IC50 of 30 nM. SNX-482 has antinociceptive effect .
S961 acetate is an high-affinity and selective insulin receptor (IR) antagonist with IC50s of 0.048, 0.027, and 630 nM for HIR-A, HIR-B, and human insulin-like growth factor I receptor (HIGF-IR) in SPA-assay, respectively .
S961 TFA is an high-affinity and selective insulin receptor (IR) antagonist with IC50s of 0.048, 0.027, and 630 nM for HIR-A, HIR-B, and human insulin-like growth factor I receptor (HIGF-IR) in SPA-assay, respectively .
GIP (1-30) amide, porcine is a full glucose-dependent insulinotropic polypeptide (GIP) receptor agonist with highaffinity equal to native GIP(1-42) . GIP (1-30) amide, porcine is a weak inhibitor of gastric acid secretion and potent stimulator of insulin.
Endotoxin inhibitor TFA is a synthetic peptide that binds lipid A with highaffinity, thereby detoxifying LPS (HY-D1056) and preventing LPS-induced cytokine release in vivo. Endotoxin inhibitor TFA inhibits the febrile response to LPS with very low toxicity and lethality .
MEN 11270, a cyclic decapeptide, is a B2 kinin receptor antagonist. MEN 11270 bound with high-affinity to the B2 kinin receptor constitutively expressed by WI38 human fibroblasts, inhibiting 3H-bradykinin (BK) with a pKi value of 10.3 .
Galanin Receptor Ligand M35 is a high-affinity ligand and antagonist of galanin receptor (Kd=0.1 nM). Galanin Receptor Ligand M35 exerts a Ki values of 0.11 and 2.0 nM for human galanin receptor type 1 and 2, respectively .
F1324 acetate is a potent, highaffinity peptidic inhibitor of B cell lymphoma 6 (BCL6), with an IC50 of 1 nM. F1324 acetate exhibits binding t1/2 value of 441 s and has strong inhibition activity against BCL6 PPI .
GIP (1-30) amide, porcine TFA is a full glucose-dependent insulinotropic polypeptide (GIP) receptor agonist with highaffinity equal to native GIP(1-42) . GIP (1-30) amide, porcine is a weak inhibitor of gastric acid secretion and potent stimulator of insulin.
Propionyl-L-carnitine is a carnitine derivative and has a highaffinity for muscular carnitine transferase. Propionyl-L-carnitine increases cellular carnitine content, thereby allowing free fatty acid transport into the mitochondria. Propionyl-L-carnitine alleviates the symptoms of PAD through a metabolic pathway, thereby improving exercise performance .
MCaE12A is a high-affinity modulator of RyR2 and increases RyR2 sensitivity to cytoplasmic calcium concentrations promoting channel opening. MCaE12A acts as an important tool for RyR2 structure-to-function studies as well as for manipulating Ca2+ homeostasis and dynamic of cardiac cell .
Kurtoxin is a selective Cav3 (T-type) voltage-gated Ca 2+ channel gating inhibitor with a Kd of 15 nM for Cav3.1 (α1G T-type) Ca 2+ channel. Kurtoxin can interact with highaffinity with native neuronal high-threshold L-type, N-type, and P-type Ca 2+ channels in central and peripheral neurons. Kurtoxin also shows cross-reactivity with voltage-gated Na + channel .
human GALP (3-32) (Galanin-like peptide (3-32)) is a potent galanin receptor agonist with highaffinity for both GalR1 (IC50=33 nM) and GalR2 (IC50=15 nM) in a competitive binding study. human GALP (3-32) exhibits the high potency in altering the extracellular acidification rate of SH-SY5Y cells transfected with GalR2 (EC50=360 nM) .
Galanin Receptor Ligand M35 TFA is a high-affinity ligand and antagonist of galanin receptor (Kd=0.1 nM). Galanin Receptor Ligand M35 TFA exerts a Ki values of 0.11 and 2.0 nM for human galanin receptor type 1 and 2, respectively .
F1324 TFA is a potent, highaffinity peptidic inhibitor of B cell lymphoma 6 (BCL6), with an IC50 of 1 nM. F1324 TFA exhibits binding t1/2 value of 441 s and has strong inhibition activity against BCL6 PPI .
SOR-C13, a carboxy-terminal truncated peptide, is a high-affinityTRPV6 antagonist with an IC50 value of 14 nM. TRPV6 is a non-voltage gated calcium channel that is associated with malignancy and poor prognosis in breast cancer. SOR-C13 has anticancer activity .
BA 1 is a potent agonist for the bombesin (BB) family of receptors. BA 1 binds with highaffinity to Bombesin receptor subtype-3 (BRS3), gastrin releasing peptide receptor (GRPR), neuromedin B receptor (NMBR) with IC50s of 6, 0.4, 2.5 nM .
(Tyr0)-Urocortin, rat is a high-affinity agonist of corticotropin-releasing factor receptor type 1 (CRF-R1) and type 2 (CRF-R2). (Tyr0)-Urocortin, rat shows inhibitory binding constants (Ki) of 1-2 nM .
APT STAT3 is a specific STAT3-binding peptide. APT STAT3 can bind STAT3 with high specificity and affinity (~231 nmol/L). APT STAT3 is a tractable agent for translation to target the broad array of cancers harboring constitutively activated STAT3 .
TAT-P4-(DATC5)2 is a high-affinity peptide inhibitor of the PICK1 (protein interacting with C kinase-1) PDZ domain, with a Ki of 1.7 nM. TAT-P4-(DATC5)2 can inhibit addiction in rats .
BA 1 TFA is a potent agonist for the bombesin (BB) family of receptors. BA1 binds with highaffinity to Bombesin receptor subtype-3 (BRS3), gastrin releasing peptide receptor (GRPR), neuromedin B receptor (NMBR) with IC50s of 6, 0.4, 2.5 nM .
GaTx2 is a seletive and a highaffinity inhibitor of ClC-2 channels with a voltage-dependent apparent KD of ∼20 pM. GaTx2 is a peptide toxin inhibitor from Leiurus quinquestriatus hebraeus venom. GaTx2 is useful in determining the role and the membrane localization of ClC-2 in specific cell types .
Prolactin-Releasing Peptide (12-31), rat is a fragment of the prolactin releasing peptide (PrRP). Prolactin-Releasing Peptide (12-31), rat shows highaffinity for GPR10 receptors. Prolactin-Releasing Peptide (12-31), stimulates calcium mobilization in CHOK1 cells transfected with the PrRP receptor .
SOR-C13 TFA, a carboxy-terminal truncated peptide, is a high-affinityTRPV6 antagonist with an IC50 value of 14 nM. TRPV6 is a non-voltage gated calcium channel that is associated with malignancy and poor prognosis in breast cancer. SOR-C13 TFA has anticancer activity .
LAH4, an alpha-helix of the designed amphipathic peptide antibiotic, exhibits potent antimicrobial, nucleic acid transfection and cell penetration activities. LAH4 possesses high plasmid DNA delivery capacities. LAH4 has a strong affinity for anionic lipids found in the outer membrane of bacterial membranes .
TAT-P4-(DATC5)2 TFA is a high-affinity peptide inhibitor of the PICK1 (protein interacting with C kinase-1) PDZ domain, with a Ki of 1.7 nM. TAT-P4-(DATC5)2 TFA can inhibit addiction in rats .
K-(D-1-Nal)-FwLL-NH2 is a highaffinity, potent and inverse ghrelin receptor agonist (EC50=3.4 nM, Ki=4.9 nM). K-(D-1-Nal)-FwLL-NH2 can be used for the research of obesity .
Biphalin TFA, a BBB-penetrable opioid peptide analog, contains two active enkephalin pharmacophores. Biphalin TFA has highaffinity for opioid receptors. Biphalin TFA shows analgesic effect in acute, neuropathic, and chronic animal pain models. Biphalin TFA is also an antiviral, antiproliferative, anti-inflammatory, and neuroprotective agent .
Prolactin Releasing Peptide (1-31), human is a highaffinityGPR10 ligand that cause the release of the prolactin. Prolactin Releasing Peptide (1-31) binds to GPR10 for human and rats with Ki values of 1.03 nM and 0.33 nM, respectively. Prolactin Releasing Peptide (1-31) can be used for the research of the hypothalamo-pituitary axis .
ELA-11(human) TFA is a highaffinity apelin receptor agonist (Ki=14 nM). ELA-11(human) TFA is a bioactive fragment of ELA-32. ELA-11(human) TFA inhibits forskolin-induced cAMP production and stimulates β-arrestin recruitment in vitro.
TPP-1 is a potent inhibitor of the PD-1/PD-L1 interaction. TPP-1 binds specifically to PD-L1 with a highaffinity (KD=95 nM). TPP-1 inhibits human tumor growth in vivo via reactivating T-cell function .
LAH4 TFA, an alpha-helix of the designed amphipathic peptide antibiotic, exhibits potent antimicrobial, nucleic acid transfection and cell penetration activities. LAH4 TFA possesses high plasmid DNA delivery capacities. LAH4 TFA has a strong affinity for anionic lipids found in the outer membrane of bacterial membranes .
Prolactin Releasing Peptide (1-31), human (acetate) is a highaffinityGPR10 ligand that causes the release of the prolactin. Prolactin Releasing Peptide (1-31) binds to GPR10 for human and rats with Ki values of 1.03 nM and 0.33 nM, respectively. Prolactin Releasing Peptide (1-31) can be used for the research of the hypothalamo-pituitary axis .
(Pro3) GIP, human TFA is an efficacious, stable and specific human GIP receptor (hGIPR) full agonist. (Pro3) GIP, human TFA has high binding affinity for human GIPR with Ki/ Kd value of 0.90 nM. (Pro3) GIP, human TFA human can be used for the research of obesity-related diabetes .
(Pro3) GIP, human ((Pro3) Gastric Inhibitory Peptide, human) is an efficacious, stable and specific human GIP receptor (hGIPR) full agonist. (Pro3) GIP, human has high binding affinity for human GIPR with Ki/ Kd values of 0.90 nM. (Pro3) GIP, human can be used for the research of obesity-related diabetes .
RVD-Hpα TFA is the N-terminally extended form of human hemopressin that acts as a selective CB1 receptor agonist. RVD-Hpα TFA increases intracellular Ca 2+ levels in cells expressing CB1 receptors in vitro. RVD-Hpα TFA also highaffinity CB2 positive allosteric modulator (Ki=50 nM).
TPP-1 TFA is a potent inhibitor of the PD-1/PD-L1 interaction. TPP-1 TFA binds specifically to PD-L1 with a highaffinity (KD=95 nM). TPP-1 TFA inhibits human tumor growth in vivo via reactivating T-cell function .
Retrocyclin-1 is a kind of Theta-defensin. Retrocyclin-1 recognizes and binds to carbohydrate-containing surface molecules, to protect cells from HIV-1 infection. Retrocyclin-1 exhibits highaffinity to fetuin, gp120 (Kd=35.4 nM), CD4 (Kd=31 nM), and galactosylceramide (Kd=24.1 nM) .
Carbetocin, an oxytocin (OT) analogue, is an oxytocin receptor agonist with a Ki of 7.1 nM. Carbetocin has highaffinity to chimeric N-terminus (E1) of the oxytocin receptor (Ki=1.17 μM). Carbetocin has the potential for postpartum hemorrhage research. Carbetocin can crosse the blood-brain barrier and produces antidepressant-like activity via activation of oxytocin receptors in the CNS .
LXW7, a cyclic peptide containing Arg-Gly-Asp (RGD), is an integrin αvβ3 inhibitor. LXW7 has a high binding affinity to αvβ3 integrin with an IC50 of 0.68 μM. LXW7 increases phosphorylation of VEGFR-2 and activation of ERK1/2. Anti-inflammatory effect .
HPV16-E711-20 epitope is a well-known HLA-A *0201-restricted human cytotoxic T lymphocyte (CTL) epitope of the HPV16 E7 protein that shows high-affinity binding to HLA-A2 in vitro. HPV16 CTL epitopes may be good candidates for the development of an effective peptide-based antitumor vaccine .
CALP2 is a calmodulin (CaM) antagonist ( (Kd of 7.9 µM)) with highaffinity for binding to the CaM EF-hand/Ca 2+-binding site. CALP2 inhibits CaM-dependent phosphodiesterase activity and increases intracellular Ca 2+ concentrations. CALP2 potently inhibits of adhesion and degranulation. CALP2 is also a strong activator of alveolar macrophages .
Apelin-12 is one of the most potent C-terminal fragments of the polypeptide that possesses a highaffinity to orphan receptor APJ receptor. Apelin-12 is involved in the regulation of body fluid homeostasis and in the central control of feeding. Apelin-12 blocks HIV-1 entry through APJ receptor. Apelin-12 exerts neuroprotective effect .
Carbetocin acetate, an oxytocin (OT) analogue, is an oxytocin receptor agonist with a Ki of 7.1 nM. Carbetocin acetate has highaffinity to chimeric N-terminus (E1) of the oxytocin receptor (Ki=1.17 μM). Carbetocin acetate has the potential for postpartum hemorrhage research. Carbetocin acetate can crosse the blood-brain barrier and produces antidepressant-like activity via activation of oxytocin receptors in the CNS .
LXW7 TFA, a cyclic peptide containing Arg-Gly-Asp (RGD), is an integrin αvβ3 inhibitor. LXW7 has a high binding affinity to αvβ3 integrin with an IC50 of 0.68 μM. LXW7 TFA increases phosphorylation of VEGFR-2 and activation of ERK1/2. Anti-inflammatory effect .
WL47, a high-affinitycavolin-1 (CAV1) ligand (Kd=23 nM), is a potent disrupter of CAV1 oligomers. WL47 shows selectivity for CAV1 over BSA, casein and HEWL. WL47 is 80% smaller in length than the original T20 (HY-P0052) parent sequence and can be used for the study of caveolin-1 function .
K-(D-1-Nal)-FwLL-NH2 TFA is a highaffinity and potent ghrelin receptor inverse agonist (Ki values are 4.9 and 31 nM in COS7 and HEK293T cells, respectively). K-(D-1-Nal)-FwLL-NH2 blocks ghrelin receptor-mediated Gq- and G13-dependent signaling pathways.
CALP2 TFA is a calmodulin (CaM) antagonist (Kd of 7.9 µM) with highaffinity for binding to the CaM EF-hand/Ca 2+-binding site. CALP2 TFA inhibits CaM-dependent phosphodiesterase activity and increases intracellular Ca 2+ concentrations. CALP2 TFA potently inhibits of adhesion and degranulation. CALP2 TFA is also a strong activator of alveolar macrophages .
Margatoxin, an alpha-KTx scorpion toxin, is a highaffinity inhibitor of Kv1.3 (Kd=11.7 pM). Margatoxin inhibits the Kv1.2 (Kd=6.4 pM) and Kv1.1 (Kd=4.2 nM). Margatoxin, a 39 amino-acid-long peptide, is isolated from the venom of the scorpion Centruroides margaritatus and widely used in ion channel research .
WL47 TFA, a high-affinitycavolin-1 (CAV1) ligand (Kd=23 nM), is a potent disrupter of CAV1 oligomers. WL47 TFA shows selectivity for CAV1 over BSA, casein and HEWL. WL47 TFA is 80% smaller in length than the original T20 (HY-P0052) parent sequence and can be used for the study of caveolin-1 function .
Orexin A (human, rat, mouse) (Hypocretin-1 (human, rat, mouse)), a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A (human, rat, mouse) is a specific, high-affinity agonist for G-protein-coupled receptor OX1R. Orexin A (human, rat, mouse) has a role in the regulation of feeding behavior. Orexin A (human, rat, mouse) is an effective anti-nociceptive and anti-hyperalgesic agent in mice and rats .
Ac-Tyr(PO3H2)-Glu-Glu-Ile-Glu-OH (compound 1) is a high-affinity pentapeptide to bind to the src SH2 domain (IC50≈1 µM). Ac-Tyr(PO3H2)-Glu-Glu-Ile-Glu-OH is an inhibitor for src SH3-SH2:phosphoprotein interactions .
Cyclo(Arg-Gly-Asp-D-Phe-Cys) (Cyclo RGDfC), a cyclic RGD peptide which has highaffinity to αvβ3, can disrupt cell integrin interactions. Cyclo(Arg-Gly-Asp-D-Phe-Cys) inhibits pluripotent marker expression in embryonic stem cells (ESCs) and the tumorigenic potential of mESCs in vivo. Cyclo(Arg-Gly-Asp-D-Phe-Cys) can be used in the research of tumors .
Cyclo(Arg-Gly-Asp-D-Phe-Cys) (Cyclo RGDfC) TFA, a cyclic RGD peptide which has highaffinity to αvβ3, can disrupt cell integrin interactions. Cyclo(Arg-Gly-Asp-D-Phe-Cys) TFA inhibits pluripotent marker expression in embryonic stem cells (ESCs) and the tumorigenic potential of mESCs in vivo. Cyclo(Arg-Gly-Asp-D-Phe-Cys) TFA can be used in the research of tumors .
Margatoxin TFA, an alpha-KTx scorpion toxin, is a highaffinity inhibitor of Kv1.3 (Kd=11.7 pM). Margatoxin TFA inhibits the Kv1.2 (Kd=6.4 pM) and Kv1.1 (Kd=4.2 nM). Margatoxin TFA, a 39 amino-acid-long peptide, is isolated from the venom of the scorpion Centruroides margaritatus and widely used in ion channel research .
Orexin A (human, rat, mouse) (Hypocretin-1 (human, rat, mouse)) TFA, a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A (human, rat, mouse) TFA is a specific, high-affinity agonist for G-protein-coupled receptor OX1R. Orexin A (human, rat, mouse) TFA has a role in the regulation of feeding behavior. Orexin A (human, rat, mouse) TFA is an effective anti-nociceptive and anti-hyperalgesic agent in mice and rats .
pm26TGF-β1 peptide is a peptide that mimics a portion of the human TGF-β1 molecule. pm26TGF-β1 peptide shows highaffinity for the TGF-β1 receptor. pm26TGF-β1 peptide displays potent anti-inflammatory properties and does not exhibit neutrophils’ chemoattraction .
pm26TGF-β1 TFA peptide is a peptide that mimics a portion of the human TGF-β1 molecule. pm26TGF-β1 peptide TFA shows highaffinity for the TGF-β1 receptor. pm26TGF-β1 peptide TFA displays potent anti-inflammatory properties and does not exhibit neutrophils’ chemoattraction .
GR231118, an analogue of the C-terminus of neuropeptide Y, is a potent , competitive and relative seletive antagonist at human neuropeptide Y Y receptor with a pKi of 10.4. GR231118 a potent agonist at the human neuropeptide Y Y4 receptor (pEC50=8.6; pKi=9.6) and a weak agonist at the human and rat neuropeptide YY2 and Y5 receptors. GR231118 also has highaffinity for the mouse neuropeptide Y Y6 receptor (pKi= 8.8) .
GR231118 TFA, an analogue of the C-terminus of neuropeptide Y, is a potent , competitive and relative seletive antagonist at human neuropeptide YY receptor with a pKi of 10.4. GR231118 a potent agonist at the human neuropeptide YY4 receptor (pEC50=8.6; pKi=9.6) and a weak agonist at the human and rat neuropeptide Y Y2 and Y5 receptors. GR231118 also has highaffinity for the mouse neuropeptide YY6 receptor (pKi= 8.8) .
Ac-Tyr(PO3H2)-Glu-Glu-Ile-Glu-OH TFA (compound 1) is a high-affinity pentapeptide to bind to the src SH2 domain (IC50≈1 µM). Ac-Tyr(PO3H2)-Glu-Glu-Ile-Glu-OH TFA is an inhibitor for src SH3-SH2:phosphoprotein interactions .
NF(N-Me)GA(N-Me)IL is a biological active peptide. (This amino acids 22 to 27 fragment is a modification of the human islet amyloid polypeptide hIAPP (NFGAIL) with N-methylation of the amide bonds at G24 and I26. The introduction of two N-methyl rests in the amyloid-core-containing sequence NFGAIL converts this amyloidogenic and cytotoxic sequence into non-amyloidogenic and non-cytotoxic peptide. The peptide is able to bind with high-affinity full-length hIAPP and to inhibit its fibrillogenesis.)
Lei-Dab7 TFA is a highaffinity, selective KCa2.2 (SK2) channel blocker (Kd=3.8 nM). Lei-Dab7 TFA exhibits >200-fold selectivity for KCa2.2 over KCa2.1, KCa2.3, KCa3.1, Kv and Kir2.1. Lei-Dab7 TFA increases theta-burst responses and increases LTP in rat hippocampal slices in vitro.
Apelin-36(human) is an endogenous orphan G protein-coupled receptor APJ agonist, with an EC50 of 20 nM. Apelin-36(human) shows highaffinity to human APJ receptors expressed in HEK 293 cells (pIC50=8.61). Apelin-36 has been linked to two major types of biological activities: cardiovascular and metabolic. Apelin-36(human) inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ .
SARS-CoV-2-IN-34 (S-20-1) is a blood brain barrier penetrable pan-coronavirus (CoV) fusion inhibitor with broad-spectrum inhibitory activity. SARS-CoV-2-IN-34 effectively inhibits infection by pseudotyped and authentic SARS-CoV-2, and pseudotyped variants of concern (VOCs). SARS-CoV-2-IN-34 shows highaffinity to RBD in S1 and HR1 domain in S2 of SARS-CoV-2 S protein. SARS-CoV-2-IN-34 can be used for the research of infection .
Apelin-36(human) TFA is an endogenous orphan G protein-coupled receptor APJ agonist, with an EC50 of 20 nM. Apelin-36(human) TFA shows highaffinity to human APJ receptors expressed in HEK 293 cells (pIC550=8.61). Apelin-36(human) TFA has been linked to two major types of biological activities: cardiovascular and metabolic. Apelin-36(human) TFA inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ .
ELA-32(human) TFA is a potent, highaffinity apelin receptor agonist (IC50=0.27 nM; Kd=0.51 nM). ELA-32(human) TFA exhibits no binding GPR15 and GPR25. ELA-32(human) TFA activates the PI3K/AKT pathway and promotes self-renewal of hESCs via cell-cycle progression and protein translation. ELA-32(human) TFA also potentiates the TGFβ pathway, priming hESCs toward the endoderm lineage. ELA-32(human) TFA stimulates angiogenesis in HUVEC cells.
SFNGGP-NH2 is a biological active peptide. (PAR-3 is a high-affinity thrombin receptor. PAR-3 mRNA is expressed in the cutaneous mast cells of humans. Protease-Activated Receptors (PARs) have been studied for their roles in itch and their itch-associated response through histamine-dependent/independent pathways have been reported. PAR-3 has been shown not to induce itching alone but possibly in conjunction with PAR-4. Co-expression of PAR-3 and PAR-4 enhances thrombin action suggesting that PAR-3 alone does not mediate transmembrane signaling but instead functions as a cofactor to activate PAR-4.)
MCE High-Affinity Iodoacetyl Agarose, a 4% highly cross-linked agarose reagent coupled with a derivative of iodoacetic acid, is ideal for conjugating sulfhydryl-containing peptide or protein for subsequent affinity purification.
MCE Anti-GFP Affinity Gel is produced through the covalent coupling of high-quality GFP antibody with agarose. It boasts a high loading capacity, exceptional specificity, and stability. This gel can be used for the detection and purification of GFP, EGFP, and their fusion-expressed proteins. Moreover, it can be utilized for cimmunoprecipitation (IP) assays without binding to BFP-tagged proteins.
Ligelizumab (QGE 031) is a humanized high-affinity monoclonal anti-IgE antibody. Ligelizumab can be used for the research of chronic spontaneous urticarial .
Carlumab (CNTO 888) is a human anti-CCL2 (chemokine ligand 2) antibody with highaffinity. Carlumab can be used in cancer research, particularly in prostate cancer .
Linavonkibart (SRK 181) is a high-affinity, fully human antibody that selectively binds to latent TGFβ1 and inhibits its activation. Linavonkibart plays an important role in cancer .
Namilumab (AMG203) is a human IgG1 monoclonal antibody that binds with highaffinity to the GM-CSF ligand, potently neutralizing GM-CSF. Namilumab can be used for the research of rheumatoid arthritis .
Rozanolixizumab (UCB7665), a humanized high-affinity anti-human neonatal Fc receptor (FcRn) monoclonal antibody (IgG4P), is used to the research of reducing pathogenic IgG in autoimmune and alloimmune diseases .
Bentracimab (PB 2452) is a neutralizing monoclonal antibody that binds Ticagrelor (HY-1006) and its major active circulating metabolite with highaffinity. Bentracimab can rapidly reverse the antiplatelet effect of Ticagrelor .
Camrelizumab (SHR-1210) is a potent humanied high-affinity IgG4-κ monoclonal antibody (mAb) to PD-1. Camrelizumab binds PD-1 at a highaffinity of 3 nM and inhibits the binding interaction of PD-1 and PD-L1 with an IC50 of 0.70 nM. Camrelizumab acts as anti-PD-1/PD-L1 agent and can be used for cancer research, including NSCLC, ESCC, Hodgkin lymphoma, and advanced HCC et,al .
Camoteskimab (AVTX-007) is a fully human, high-affinity anti-IL-18 monoclonal antibody. Camoteskimab has the potential for the autoinflammatory diseases research, including adult-onset Still’s disease (AOSD) .
Elarekibep (PRS-060) (AZD1402) is a highaffinity, slowly dissociating, long-acting full antagonist of IL-4Ra. Elarekibep can be used for the research of T2 endotype asthma .
Nesvacumab is a fully human immunoglobulin G1 (IgG1) monoclonal antibody that specifically binds and inactivates the Tie2 receptor ligand Angiopoietin-2 (Ang2) with highaffinity, but shows no binding to Ang1 .
Ravulizumab (ALXN1210) is a humanized monoclonal antibody that specifically binds with highaffinity to the human complement protein C5. Ravulizumab can be used for the research of paroxysmal nocturnal hemoglobinuria, atypical hemolytic uremic syndrome, and myasthenia gravis .
Axatilimab (SNDX-6352) is a humanized IgG4 antibody with highaffinity to CSF-1R. Axatilimab can be used for the research of chronic graft versus host disease (cGVHD) and neoplastic diseases .
Tralokinumab, a fully human IgG4 monoclonal antibody, specifically binds with highaffinity to IL-13 alone, preventing its interaction with the receptor and subsequent downstream signalling. Tralokinumab can be used for the research of the atopic dermatitis (AD) .
Telisotuzumab (ABT-700) is a human recombinant bivalent antibody, a therapeutic antibody against the hepatocyte growth factor receptor (MET) that binds c-Met with highaffinity and inhibits c-Met signaling. Telisotuzumab has antitumor activity .
Secukinumab (AIN457) is a highaffinity, human monoclonal antibody targeted against interleukin (IL)-17A. Secukinumab is the first-in-class anti-IL-17 agent used for the research of plaque psoriasis, ankylosing spondylitis and psoriatic arthritis .
Fresolimumab (GC1008) is a high-affinity fully human monoclonal antibody that neutralizes the active form of human TGFβ1, TGFβ2, and TGFβ3. Fresolimumab can be used for the research of cancer and fibrotic diseases .
Abelacimab (MAA868) is a fully human IgG1 monoclonal antibody that binds with highaffinity to the catalytic structural domain of FXI and locks it in the zymogen conformation, thereby preventing its activation by FXIIa or thrombin. Abelacimab can be used in thromboembolic disease studies .
CC-90002 is a humanized anti-CD47 monoclonal antibody (mAb). CC-90002 has a highaffinity for binding to CD47 with a subnanomolar Kd value. CC-90002 can be used for the research of hematologic malignancies and solid tumors .
Farletuzumab (MORAb-003) is a potent folate receptor-alpha (FRα) inhibitor. Farletuzumab is a humanized monoclonal antibody with highaffinity for FRα. Farletuzumab possesses growth-inhibitory functions on cells overexpressing FRα. Farletuzumab can be used in research of cancer .
Pozelimab (REGN3918) is a fully human IgG4 anti-C5 monoclonal antibody. Pozelimab binds to C5 and C5 variants with highaffinity and blocks complement-mediated hemolysis. Pozelimab can be used for the research of complement-mediated diseases .
KWAR23 is an anti-human SIRPα antibody. KWAR23 binds human SIRPα with highaffinity and disrupts its binding to CD47. KWAR23 shows antitumor activity in combination with tumor-opsonizing antibodies and can be used in cancer immunotherapy research .
Narsoplimab (OMS 721) is a high-affinity fully human immunoglobulin gamma 4 (IgG4) monoclonal antibody that binds MASP-2 and blocks lectin pathway activation. Narsoplimab can be used in research of hematopoietic stem-cell transplantation and SARS-CoV-2 .
Sabatolimab (MBG453) is a high-affinity, humanized, IgG4 (S228P) antibody targeting TIM-3, an inhibitory receptor that regulates adaptive and innate immune responses. Sabatolimab is a potential immunosuppression agent that can target TIM-3 on immune and myeloid cells .
Imsidolimab (ANB 019) is a high-affinity, humanized monoclonal antibody of anti-IL-36R. Imsidolimab antagonizes IL-36 cytokine signal transduction. Imsidolimab has potential application in generalized pustular psoriasis (GPP) and other inflammatory skin diseases .
Ociperlimab is a humanized IgG1 anti-TIGIT antibody. Ociperlimab binds to the extracellular domain of human TIGIT with highaffinity (KD = 0.135 nM). Ociperlimab blocks the interaction between TIGIT and its ligands PVR or PVR-L2. Ociperlimab can be used in research of cancer .
Tuvirumab (OST 577; SDZ-OST 577) is a human IgG1 subclass monoclonal antibody directed against HBV surface antigen (HBsAg). Tuvirumab binds specifically and with highaffinity (K=3.6 nM) to HBsAg. Tuvirumab has the potential for chronic hepatitis B research .
Emapalumab (NI-0501) is a human monoclonal IgG1 antibody that noncompetitively inhibits IFN-γ. Emapalumab binds with highaffinity (Kd= 1.4 pM) to both free IFN-γ as well as IFN-γ bound to its receptor. Emapalumab can be used in research of hemophagocytic lymphohistiocytosis (HLH) .
Bleselumab (ASKP 1240) is a human anti-CD40 monoclonal antibody (mAb). Bleselumab binds to human CD40 with highaffinity (Kd: 0.24 nM). Bleselumab inhibits immune responses by blocking the interaction of CD40 with its ligand CD40L. Bleselumab prevents organ transplant rejection .
Clazakizumab is a monoclonal antibody with highaffinity and specificity for the IL-6 (interleukin-6) cytokine. Clazakizumab may be helpful in inhibiting the cytokine response to SARS-CoV-2 in COVID-19. Clazakizumab can be used for the research of psoriatic arthritis (PsA) and renal antibody-mediated rejection .
Tanezumab (RN-624) is a humanized anti-NGF mAb with highaffinity and specificity. Tanezumab blocks NGF binding to its receptors, p75 and TrkA, in the peripheral nervous system. Tanezumab can be used in studies of acute and chronic pain such as osteoarthritis, knee and neuralgia, as well as post-herpetic neuralgia .
Abrezekimab (VR 942) contains CDP7766, a humanized, high-affinity, neutralizing, anti-human-IL-13 antibody fragment that binds to IL-13. Abrezekimab prevents binding to the IL-13Rα1 subunit. Abrezekimab can be used in research of asthma .
Latozinemab (AL001) is a recombinant human anti-Sortilin monoclonal antibody. Latozinemab effectively binds Sortilin with a highaffinity and blocks the interaction between progranulin protein (PGRN) and Sortilin receptor. Latozinemab has the potential for progranulin gene (GRN) mutations causative of Frontotemporal dementia (FTD) (FTD-GRN) research .
Anti-MERS-3A1 mAb (MERS-3A1) is a human monoclonal IgG1 antibody with the high binding affinity produced in CHO cells.
Anti-MERS-3A1 mAb bocks the binding of MERS-CoV spike protein to DPP4 receptor .
Dostarlimab (TSR-042) is a humanized anti-PD-1 monoclonal antibody. Dostarlimab binds with highaffinity to human PD-1 and competitively inhibits its interaction with its ligands, PD-L1 and PD-L2, with IC50s of 1.8 and 1.5 nM, respectively .
Tislelizumab, a monoclonal antibody with high binding affinity to the PD-1 receptor, minimizes Fcγ receptor binding on macrophages, thereby abrogating antibody-dependent phagocytosis, a mechanism of T cell clearance and potential resistance to anti-PD-1 research. Tislelizumab can be used for the research of advanced squamous non-small-cell lung cancer .
Cemiplimab (Anti-Human PD-1) is a high-affinity programmed death receptor-1 (PD-1) monoclonal IgG4 antibody that blocks PD-1/PD-L1-mediated T-cell suppression. Cemiplimab is commonly used in squamous cell skin cancer research .
Tildrakizumab (SCH 900222) is a humanized anti-IL-23 (p19 subunit) monoclonal antibody. IL-23 is a critical cytokine to maintain the Th17 cell phenotype. Tildrakizumab has high-affinity for single-chain IL-23 (Kd: 136 pM). Tildrakizumab is effective against moderate to severe plaque psoriasis .
Zalutumumab is a highaffinity, completely human IgG1 monoclonal antibody targeting EGFR. Zalutumumab binds to domain III of the EGF receptor and acts by blocking the binding of EGF and by sterically interfering with the active conformation of the receptor. Zalutumumab binds with IgG and its Fab fragment with EC50s of 7 and 19 nM, respectively. Zalutumumab can be used for the research of cancer .
Surzebiclimab (BGB-A425) is a humanized IgG1-variant monoclonal antibody against T-cell immunoglobulin and mucin-domain containing-3 (TIM-3). Surzebiclimab binds to the extracellular domain of human Tim-3 with highaffinity (KD=0.36 nM) and specificity. Surzebiclimab can be used in research of cancer .
Reslizumab (Sch 55700) is humanized monoclonal antibodies that target interleukin-5 (IL-5) for the treatment of eosinophilic asthma. Reslizumab is effective in neutralizing the function of IL-5. Reslizumab has high binding affinity for human IL-5, with KD values of 109 pM and 4.3 pM in the the Biacore surface plasmon resonance and Kinetic Exclusion Assay, respectively .
Sarilumab (Anti-Human IL6Rα, Human Antibody) is a human immunoglobulin G1 monoclonal antibody. Sarilumab, a interleukin-6 (IL-6) receptor antagonist, binds to the IL-6 receptor with highaffinity and inhibits cis and trans signaling by IL-6, resulting in reduced inflammation. Sarilumab can be used for the research of Rheumatoid arthritis .
Daclizumab (Zenapax) is a humanized, monoclonal antibody that blocks CD25 (α-subunit of the high-affinity interleukin-2 receptor (IL-2R-HA)). Daclizumab (Zenapax) reversibly binds to CD25and prevents the interaction of IL-2 with the IL-2R-HA. Daclizumab (Zenapax) can be used for multiple sclerosis research .
Abicipar pegol (AGN-150998, MP0112) is an anti-VEGF DARPin molecule, a novel class of small proteins containing ankyrin repeat domains engineered to bind with high specificity and affinity to target proteins. Abicipar pegol effectively inhibits angiogenesis and vascular permeability and is used in the study of diseases related to ocular inflammation by intravitreal injection, reducing mean retinal thickness and leakage area .
Stamulumab (MYO-029) is a recombinant human IgG1λ antibody that binds to myostatin and neutralizes its activity by preventing binding to its endogenous high-affinity receptor ActRIIB. Stamulumab leads to muscle fiber hypertrophy and not hyperplasia in SCID mice. Stamulumab has the potential for Becker muscular dystrophy (BMD), facioscapulohumeral dystrophy (FSHD), and limb-girdle muscular dystrophy (LGMD) research .
Emactuzumab(RG 7155) is a specific monoclonal antibody that inhibits colonystimulating factor 1 receptor (CSF1R) activation. Emactuzumab has highaffinity for CSF-1R with Ki value of 0.2 nM to blocks CSF-1R dimerization. Emactuzumab can be used for the research of several diseases, such as diffuse-type tenosynovial giant cell tumour (dt-GCT) .
TSR-033 is a highaffinity human IgG4 antibody targeting LAG-3 (lymphocyte activation gene-3), a co-receptor associated with impaired T cell function and often co-expressed with PD-1, that enhances T cell function and PD-1 blocking activity in vitro and in vivo. TSR-033 has anti-tumor activity .
Anzurstobart (CC-95251; BMS-986351) is a high-affinity, fully human monoclonal anti-SIRPα antibody that blocks the binding of CD47 to SIRPα. Anzurstobart enhances macrophage phagocytic activity against DLBCL cell lines in co-culture models when combined with the antibody Rituximab (HY-P9913). Anzurstobart has the potential for solid and hematologic malignancies research .
Cixutumumab (IMC-A12) is a human anti-IGF-1R monoclonal antibody with highaffinity that inhibits ligand-dependent receptor activation and downstream signaling. Cixutumumab also mediates the internalization and degradation of IGF-IR. Cixutumumab shows broad-spectrum anti-tumour activity and can be used in studies of cancers such as lung cancer, malignancies, leukaemia, non-small cell lung cancer and prostate cancer .
Suvratoxumab (MEDI4893) is a long-acting, high-affinityhuman anti-α-toxin monoclonal antibody (IgG1κ type). Suvratoxumab potently neutralizes α-toxin, a key S. aureus virulence factor. Suvratoxumab improves survival and reduces lung injury in an immunocompromised mice model of pneumonia. Suvratoxumab also enhances the antibacterial activity of Vancomycin (HY-B0671) or Linezolid (HY-10394) .
Cosibelimab (CK-301; TG-1501) is a high-affinity, fully human PD-L1-blocking monoclonal antibody that binds PD-L1 and blocks its interaction with PD-1. Cosibelimab has a functional Fc domain and is capable of inducing ADCC and complement-dependent cytotoxicity (CDC)-mediated killing of PD-L1 + cell lines, including lymphoma cells .
Tebentafusp (IMCgp100) is a bispecific fusion protein to target gp100 peptide-HLA-A*02:01 (a melanoma-associated antigen). Tebentafusp guides T cells to kill gp100-expressing tumor cells via a highaffinity T-cell receptor (TCR) binding domain and an anti-CD3 T-cell engaging domain. Tebentafusp leads to inflammatory cytokines and cytolytic proteins production, resulting in the direct lysis of tumour cells .
Cendakimab (RPC4046; ABT 308; CC-93538) is a selective, humanized, recombinant monoclonal antibody against the IL-13 molecule. Cendakimab has a highaffinity and potency for both human wild-type and variant IL-13 and blocks binding of IL-13 to both IL-13Rα1 and IL-13Rα2 with IC50s of 352 pM and 631 pM by ELISA, respectively. Cendakimab recognizes both wild-type human IL-13 and the common polymorphic variant R110Q, with binding affinities of 52 and 50 pM, respectively. Cendakimab has the potential for IL-13-related allergic/inflammatory diseases (e.g., asthma and eosinophilic esophagitis) .
Izeltabart is a high-affinity humanized antibody targeting ADAM9. Izeltabart can be used as ADC Antibody for site-specific conjugation with Maytansinoid-based DM21-C (a Drug-Linker Conjugates for ADC), to synthesize IMGC936 (Antibody-Drug Conjugates (ADCs)) with strong anti-cancer activity. DM21-C is composed of Maytansinoid (microtubule inhibitor) and a stable tripeptide linker. IMGC936 exhibits cytotoxicity against ADAM9-positive human tumor cell lines and potent antitumor activity in xenograft tumor models .
Cinrebafusp alfa (PRS 343) is a highaffinityCD137/HER2 bispecfic anticalin-based drug. Cinrebafusp alfa binds to recombinant human HER2 (Kd=0.3 nM) and human monomeric CD137 (4-1BB; Kd=5 nM). Cinrebafusp alfa facilitates T-cell costimulation by tumor-localized, HER2-dependent 4-1BB clustering and activation, further enhancing T-cell receptor-mediated activity and leading to tumor destruction. Cinrebafusp alfa has the potential for HER2+ solid tumors research .
Endomorphin 1, a highaffinity, highly selective agonist of the μ-opioid receptor (Ki: 1.11 nM), displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM. Endomorphin 1 has antinociceptive properties .
Harmine Hydrochloride (Telepathine Hydrochloride) is a natural DYRK inhibitor with anticancer and anti-inflammatory activities. Harmine has a highaffinity of 5-HT2A serotonin receptor, with an Ki of 397 nM .
Crocetin (Transcrocetin), extracted from saffron (Crocus sativus L.), acts as an NMDA receptor antagonist with highaffinity . Crocetin is capable of crossing the blood-brain barrier and reach the central nervous system (CNS) .
Estradiol 17-(β-D-Glucuronide), a metabolite of estrogen, is well known to cause intrahepatic cholestasis in humans. Estradiol 17-(β-D-Glucuronide) is a high-affinity substrate for oatp organic anion transporter .
β-Endorphin, equine TFA is an endogenous opioid peptide, which binds at highaffinity to both μ/δ opioid receptors. β-Endorphin, equine TFA has analgesic properties .
Epi-cryptoacetalide is a natural diterpenoid. Epi-cryptoacetalide reveals highaffinity to ER-α and PGE2 receptor (EP2 subtype) with Ki values of 0.3 μM and 1.92 μM, respectively. Epi-cryptoacetalide has anti-endometriosis activities .
Propionyl-L-carnitine is a carnitine derivative and has a highaffinity for muscular carnitine transferase. Propionyl-L-carnitine increases cellular carnitine content, thereby allowing free fatty acid transport into the mitochondria. Propionyl-L-carnitine alleviates the symptoms of PAD through a metabolic pathway, thereby improving exercise performance .
N-Methylcytisine (Caulophylline), a tricyclic quinolizidine alkaloid, exerts hypoglycaemic, analgesic and anti-inflammatory activities. N-methylcytisine is a selective ligand of nicotinic receptors of acetylcholine in the central nervous system and has a highaffinity (Kd = 50 nM) to nicotinic acetylcholine receptors (nAChR) from squid optical ganglia .
2',3'-cGAMP sodium (2'-3'-cyclic GMP-AMP sodium) is a endogenous cGAMP in mammalian cells. 2',3'-cGAMP sodium binds to STING with a highaffinity and is a potent inducer of interferon-β (IFNβ). 2',3'-cGAMP sodium is produced in mammalian cells in response to DNA in the cytoplasm .
Sialyl-Lewis X (sLeX) is a sialylated fucosylated tetrasaccharide, an endogenous antigen. Sialyl-Lewis X is a high-affinityligand for selectins (E-, P-, and L-selectin) . Sialyl-Lewis X binds to ELAM-1 and CD62 and has the ability to inhibits CD62-mediated neutrophil recruitment to sites of inflammation .
Deoxyneocryptotanshinone, a natural tanshinone, is a highaffinityBACE1 (Beta-secretase) inhibitor with an IC50 value of 11.53 μM. Deoxyneocryptotanshinone shows a promising dose-dependent inhibition of protein tyrosine phosphatase 1B (PTP1B) with an IC50 value of 133.5 μM. Deoxyneocryptotanshinone can be used for Alzheimer's disease research .
(6S)-Tetrahydrofolic acid is 1000-fold more active than the (6R) form at promoting the binding of fluorodeoxyuridylate to thymidylate synthase and 600-fold more active as a growth factor of P. cerevisiae. (6S)-Tetrahydrofolic acid also has a low affinity and high dissociation rate for folate-binding protein .
Pulcherriminic acid is a cyclic dipeptide antimicrobial agent with highaffinity for Fe 3+, found mainly in Bacillus and yeast. Pulcherriminic acid chelates iron ions through a non-enzymatic reaction to form the extracellular red pigment pulcherrimin, which competes for iron nutrition and thus achieves an antibacterial effect. Pulcherriminic acid has great applications in food, agriculture and medical industries .
Propranolol hydrochloride is a nonselective β-adrenergic receptor (βAR) antagonist, has highaffinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively . Propranolol hydrochloride inhibits [ 3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM . Propranolol hydrochloride is used for study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy .
Propranolol is a nonselective β-adrenergic receptor (βAR) antagonist, has highaffinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively . Propranolol inhibits [ 3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM . Propranolol is used for the study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy .
Margatoxin, an alpha-KTx scorpion toxin, is a highaffinity inhibitor of Kv1.3 (Kd=11.7 pM). Margatoxin inhibits the Kv1.2 (Kd=6.4 pM) and Kv1.1 (Kd=4.2 nM). Margatoxin, a 39 amino-acid-long peptide, is isolated from the venom of the scorpion Centruroides margaritatus and widely used in ion channel research .
3′-Methoxyfurano[4″,5″:3,4]chalcone (compound 2) is a selective A2AAR antagonist (IC50=33.5 nM) with highaffinity. 3′-Methoxyfurano[4″,5″:3,4]chalcone is also a natural product obtained from the bark of Allium cepa L. 3′-Methoxyfurano[4″,5″:3,4]chalcone can promote T cell activation and can be used in cancer immunity research .
Ifenprodil tartrate is a typical noncompetitive NMDA receptor antagonist. Ifenprodil tartrate exerts highaffinity at NR1A/NR2B receptors (IC50=0.34 μM) over 400-fold than at NR1A/NR2A receptors (IC50=146 μM) . Ifenprodil tartrate inhibits GIRK (Kir3), reduces inward currents through the basal GIRK activity. Ifenprodil tartrate has the potential to be a cerebral vasodilator .
Brevetoxin-3 (PbTx-3) is a potent allosteric voltage-gated Na + channel activator and has multiple active centers (A-ring lactone, C-42 of R side chain) . Brevetoxin-3 (PbTx-3) has a highaffinity to site 5 of the voltage-sensitive Na + channels, inhibits the inactivation of Na + channels and prolongs the mean open time of these channels. Brevetoxin-3 (PbTx-3) repeated exposures can lead to prolonged airway hyperresponsiveness (AHR) and lung inflammation .
Pentraxin 3/TSG-14 protein is a multifunctional protein that plays a role in immune response and inflammation. It is involved in the recognition and clearance of pathogens, as well as regulation of inflammatory processes. Dysregulation of Pentraxin 3/TSG-14 protein has been associated with various diseases, including cardiovascular disorders and infections. Targeting Pentraxin 3/TSG-14 protein may hold therapeutic potential in these conditions. TrkA Protein, Human (HEK293, His) is the recombinant human-derived TrkA protein, expressed by HEK293 , with N-His labeled tag. The total length of TrkA Protein, Human (HEK293, His) is 220 a.a., with molecular weight of 35-60 kDa.
The TrkA protein is a receptor tyrosine kinase that is critical in central and peripheral nervous system development, regulating neuronal proliferation, differentiation, and survival. As a high-affinity NGF receptor, TrkA undergoes homodimerization and autophosphorylation upon ligand binding, activating downstream effectors (SHC1, FRS2, SH2B1, SH2B2, PLCG1) cascade. TrkA Protein, Rat (HEK293, His) is the recombinant rat-derived TrkA protein, expressed by HEK293 , with C-His labeled tag. The total length of TrkA Protein, Rat (HEK293, His) is 386 a.a., with molecular weight of ~70-95 kDa.
TrkA Protein (isoform 3) belongs to the nerve growth factor receptor family and can promote angiogenesis and has carcinogenic activity when overexpressed. TrkA Protein (isoform 3) antagonizes the anti-proliferative NGF-NTRK1 signaling that promotes the differentiation of neuronal precursors. TrkA Protein, Canine (HEK293, His) is the recombinant canine-derived TrkA protein, expressed by HEK293 , with N-His labeled tag. The total length of TrkA Protein, Canine (HEK293, His) is 126 a.a., with molecular weight of 27-33 kDa.
The TrkA protein is a receptor tyrosine kinase that is critical in central and peripheral nervous system development, regulating neuronal proliferation, differentiation, and survival. As a high-affinity NGF receptor, TrkA undergoes homodimerization and autophosphorylation upon ligand binding, activating downstream effectors (SHC1, FRS2, SH2B1, SH2B2, PLCG1) cascade. TrkA Protein, Rat (HEK293, Fc) is the recombinant rat-derived TrkA protein, expressed by HEK293 , with C-hFc labeled tag. The total length of TrkA Protein, Rat (HEK293, Fc) is 418 a.a., with molecular weight of 92-102 kDa.
TrkA Protein, Rabbit (HEK293, His) is a nerve growth factor (NGF) receptor that belongs to the tyrosine kinase receptor family. TRKA (NTRK1) gene encodes the high affinity receptor for a neurotrophin nerve growth factor (NGF). It is critical for the correct development of many types of neurons including pain-mediating sensory neurons and also controls proliferation, differentiation and survival of many neuronal and non-neuronal cells. TrkA Protein, Rabbit (HEK293, His) is the recombinant Rabbit-derived TrkA protein, expressed by HEK293 , with C-His labeled tag. The total length of TrkA Protein, Rabbit (HEK293, His) is 382 a.a., with molecular weight of ~43.4 kDa.
TrkA Protein (isoform 3) belongs to the nerve growth factor receptor family and can promote angiogenesis and has carcinogenic activity when overexpressed. TrkA Protein (isoform 3) antagonizes the anti-proliferative NGF-NTRK1 signaling that promotes the differentiation of neuronal precursors. TrkA Protein, Canine (HEK293, Fc) is the recombinant canine-derived TrkA protein, expressed by HEK293 , with N-hFc labeled tag. The total length of TrkA Protein, Canine (HEK293, Fc) is 126 a.a., with molecular weight of 55-61 kDa.
TrkA protein is a key receptor tyrosine kinase that guides the development and maturation of the nervous system and affects neuronal proliferation, differentiation, and survival. TrkA serves as a high-affinity receptor for NGF (its primary ligand) and also responds to NTF3/neurotropin-3. TrkA Protein, Mouse (HEK293, Fc) is the recombinant mouse-derived TrkA protein, expressed by HEK293 , with C-hFc labeled tag. The total length of TrkA Protein, Mouse (HEK293, Fc) is 420 a.a., with molecular weight of ~116 kDa.
TrkA protein is a key receptor tyrosine kinase that guides the development and maturation of the nervous system and affects neuronal proliferation, differentiation, and survival. TrkA serves as a high-affinity receptor for NGF (its primary ligand) and also responds to NTF3/neurotropin-3. TrkA Protein, Mouse (HEK293, His) is the recombinant mouse-derived TrkA protein, expressed by HEK293 , with C-His, C-8*His labeled tag. The total length of TrkA Protein, Mouse (HEK293, His) is 387 a.a., with molecular weight of ~55-125 kDa.
TrkA protein is an important receptor tyrosine kinase that regulates the development of the central and peripheral nervous systems and affects the proliferation, differentiation, and survival of neurons. As a high-affinity receptor for NGF, TrkA is activated upon NGF binding through homodimerization and autophosphorylation. TrkA Protein, Human (HEK293, His-Fc) is the recombinant human-derived TrkA protein, expressed by HEK293 , with C-hFc, C-His labeled tag. The total length of TrkA Protein, Human (HEK293, His-Fc) is 382 a.a., with molecular weight of 85-95 kDa.
CD64 protein, a high affinity receptor, mediates IgG effector functions, triggering antibody-dependent cellular cytotoxicity (ADCC). It interacts with IGHG1 and forms a signaling complex with FCERG1, contributing to immune responses. CD64 also interacts with FLNA, EPB41L2, LAT, PPL, HCK, and LYN to prevent degradation of FCGR1A and regulate immune function. CD64 Protein, Human (CHO, C-His) is the recombinant human-derived CD64 protein, expressed by CHO , with C-His labeled tag. The total length of CD64 Protein, Human (CHO, C-His) is 273 a.a., with molecular weight of 45-60 kDa.
CD64 Protein, with leukotriene receptor binding, crucially regulates processes like phagocytosis and pain perception, responding to epinephrine. Located in membrane rafts, CD64, encoded by FCGR1A, shows biased expression, especially in Spleen (RPKM 177.3) and Lung (RPKM 93.7). This emphasizes its importance in immune responses and sensory functions across diverse physiological contexts. CD64 Protein, Rat (HEK293, His) is the recombinant rat-derived CD64 protein, expressed by HEK293 , with C-His labeled tag. The total length of CD64 Protein, Rat (HEK293, His) is 269 a.a., with molecular weight of 40-42 kDa.
PDE9A is a phosphodiesterase that uniquely hydrolyzes second messengers with unparalleled specificity, particularly in the regulation of natriuretic peptide-dependent signaling in the heart, which is critical for the control of cardiac hypertrophy. Its specificity rules out effects on nitric oxide-dependent signaling in the heart. PDE9A Protein, Human (His) is the recombinant human-derived PDE9A protein, expressed by E. coli , with N-His labeled tag. The total length of PDE9A Protein, Human (His) is 326 a.a., with molecular weight of ~37 kDa.
The CD64 protein is a high-affinity receptor for the immunoglobulin gamma Fc region and plays a key role in innate and adaptive immune responses. It prevents FCGR1A degradation by interacting with FCERG1 and FLNA to form a functional signaling complex. CD64 Protein, Mouse (HEK293, His-Avi) is the recombinant mouse-derived CD64 protein, expressed by HEK293 , with C-Avi, C-His labeled tag. The total length of CD64 Protein, Mouse (HEK293, His-Avi) is 273 a.a., with molecular weight of 45-50 kDa.
The Fc epsilon RIA/FCER1A protein is a high-affinity receptor for IgE and critically mediates IgE effector function in myeloid cells. After binding to IgE and cross-linking with antigen, it activates signaling pathways that induce myeloid cell activation and differentiation. Fc epsilon RIA/FCER1A Protein, Human (His-SUMO) is the recombinant human-derived Fc epsilon RIA/FCER1A protein, expressed by E. coli , with N-6*His, N-SUMO labeled tag. The total length of Fc epsilon RIA/FCER1A Protein, Human (His-SUMO) is 180 a.a., with molecular weight of ~37 kDa.
The CD64 protein is a high-affinity receptor for the immunoglobulin gamma Fc region and plays a key role in innate and adaptive immune responses. It prevents FCGR1A degradation by interacting with FCERG1 and FLNA to form a functional signaling complex. CD64 Protein, Mouse (273a.a, HEK293, His) is the recombinant mouse-derived CD64 protein, expressed by HEK293 , with C-6*His labeled tag. The total length of CD64 Protein, Mouse (273a.a, HEK293, His) is 273 a.a., with molecular weight of 40-60 kDa.
PDE9A is a phosphodiesterase that uniquely hydrolyzes second messengers with unparalleled specificity, particularly in the regulation of natriuretic peptide-dependent signaling in the heart, which is critical for the control of cardiac hypertrophy. Its specificity rules out effects on nitric oxide-dependent signaling in the heart. PDE9A Protein, Human (sf9, His-GST) is the recombinant human-derived PDE9A protein, expressed by Sf9 insect cells , with N-His, N-GST labeled tag. The total length of PDE9A Protein, Human (sf9, His-GST) is 533 a.a., with molecular weight of ~75 kDa.
FCAMR/CD351, functioning as a receptor, exhibits high-affinity binding to the Fc fragment of IgA and IgM. It plays a role in the immune response by mediating the endocytosis of IgA and IgM during the immune response to microbes. FCAMR/CD351 Protein, Mouse (HEK293, His) is the recombinant mouse-derived FCAMR/CD351 protein, expressed by HEK293 , with C-His labeled tag. The total length of FCAMR/CD351 Protein, Mouse (HEK293, His) is 420 a.a., with molecular weight of ~46.4 KDa.
CD64 protein, a high affinity receptor, mediates IgG effector functions, triggering antibody-dependent cellular cytotoxicity (ADCC). It interacts with IGHG1 and forms a signaling complex with FCERG1, contributing to immune responses. CD64 also interacts with FLNA, EPB41L2, LAT, PPL, HCK, and LYN to prevent degradation of FCGR1A and regulate immune function. CD64 Protein, Human (Biotinylated, 272a.a, HEK293, His-Avi) is the recombinant human-derived CD64 protein, expressed by HEK293 , with C-Avi, C-His labeled tag. The total length of CD64 Protein, Human (Biotinylated, 272a.a, HEK293, His-Avi) is 272 a.a., with molecular weight of 34-68 kDa.
CD64 protein, a high affinity receptor, mediates IgG effector functions, triggering antibody-dependent cellular cytotoxicity (ADCC). It interacts with IGHG1 and forms a signaling complex with FCERG1, contributing to immune responses. CD64 also interacts with FLNA, EPB41L2, LAT, PPL, HCK, and LYN to prevent degradation of FCGR1A and regulate immune function. CD64 Protein, Human (Cell-Free, His) is the recombinant human-derived CD64 protein, expressed by E. coli Cell-free , with N-10*His labeled tag. The total length of CD64 Protein, Human (Cell-Free, His) is 359 a.a., with molecular weight of 46.9 kDa.
The CD64 protein is a high-affinity receptor for the immunoglobulin gamma Fc region and plays a key role in innate and adaptive immune responses. It prevents FCGR1A degradation by interacting with FCERG1 and FLNA to form a functional signaling complex. CD64 Protein, Rabbit (HEK293, His) is the recombinant Rabbit-derived CD64 protein, expressed by HEK293 , with C-His labeled tag. The total length of CD64 Protein, Rabbit (HEK293, His) is 291 a.a., with molecular weight of ~32.2 KDa.
IL-2R beta (CD122), a type Ⅰ cytokine receptor expressed on T lymphocytes, is a receptor for IL-2 (Kd: 1 nM approximately). IL-2R beta mediates T cell immune responses, such as stimulating T cell proliferation and activating lymphokine-activated killer cells. IL-2R beta/CD122 Protein, Canine (HEK293, Fc) is a recombinant canine IL-2R beta (M1-P244) with a C-Terminal hFc tag, which is produced in HEK293 cells.
IL-2R beta (CD122), a type Ⅰ cytokine receptor expressed on T lymphocytes, is a receptor for IL-2 (Kd: 1 nM approximately). IL-2R beta mediates T cell immune responses, such as stimulating T cell proliferation and activating lymphokine-activated killer cells. IL-2R beta/CD122 Protein, Rat (HEK293, His) is a recombinant rat IL-2R beta (M1-E239) with a C-Terminal His tag, which is produced in HEK293 cells.
IL-2R beta (CD122), a type Ⅰ cytokine receptor expressed on T lymphocytes, is a receptor for IL-2 (Kd: 1 nM approximately). IL-2R beta mediates T cell immune responses, such as stimulating T cell proliferation and activating lymphokine-activated killer cells. IL-2R beta/CD122 Protein, Rhesus Macaque (HEK293, Fc) is a recombinant Rhesus Macaque IL-2R beta (M1-D239) with a C-Terminal hFc tag, which is produced in HEK293 cells.
IL-2R beta (CD122), a type Ⅰ cytokine receptor expressed on T lymphocytes, is a receptor for IL-2 (Kd: 1 nM approximately). IL-2R beta mediates T cell immune responses, such as stimulating T cell proliferation and activating lymphokine-activated killer cells. IL-2R beta/CD122 Protein, Rhesus Macaque (HEK293, His) is a recombinant Rhesus Macaque IL-2R beta (M1-D239) with a C-Terminal His tag, which is produced in HEK293 cells.
CXCR2 protein acts as a receptor for interleukin-8 and induces neutrophil activation through the G protein-mediated phosphatidylinositol-calcium second messenger system. In addition to IL-8, CXCR2 also exhibits high-affinity binding to ligands such as CXCL3, GRO/MGSA, and NAP-2. CXCR2 Protein, Mouse (Cell-Free, His) is the recombinant mouse-derived CXCR2 protein, expressed by E. coli Cell-free , with N-10*His labeled tag. The total length of CXCR2 Protein, Mouse (Cell-Free, His) is 359 a.a., with molecular weight of 43.2 kDa.
IL-2R beta (CD122), a type Ⅰ cytokine receptor expressed on T lymphocytes, is a receptor for IL-2 (Kd: 1 nM approximately). IL-2R beta mediates T cell immune responses, such as stimulating T cell proliferation and activating lymphokine-activated killer cells. IL-2R beta/CD122 Protein, Human (HEK293, Fc) is a recombinant human extracellular region of IL-2R beta (A27-D239) with a C-Terminal Fc tag, which is produced in HEK293 cells.
IL-2R beta (CD122), a type Ⅰ cytokine receptor expressed on T lymphocytes, is a receptor for IL-2 (Kd: 1 nM approximately). IL-2R beta mediates T cell immune responses, such as stimulating T cell proliferation and activating lymphokine-activated killer cells. IL-2R beta/CD122 Protein, Mouse (P.pastoris, His) is a recombinant mouse IL-2R beta (27A-240E) with a N-Terminal His tag, which is produced in P.pastoris.
IL-2R beta (CD122), a type Ⅰ cytokine receptor expressed on T lymphocytes, is a receptor for IL-2 (Kd: 1 nM approximately). IL-2R beta mediates T cell immune responses, such as stimulating T cell proliferation and activating lymphokine-activated killer cells. IL-2R beta/CD122 Protein, Human (HEK293, His) is a recombinant human extracellular region of IL-2R beta (A27-D239) with a C-Terminal 6*His tags, which is produced in HEK293 cells.
The SLC31A1 protein is an important uniporter that can transport copper(1+) from the extracellular space into the cytoplasm with remarkable specificity and deliver it directly to molecular chaperones such as ATOX1. This process tightly regulates intracellular copper(1+) levels and may be involved in intestinal copper absorption. SLC31A1 Protein, Human (Cell-Free, His-SUMO) is the recombinant human-derived SLC31A1 protein, expressed by E. coli Cell-free , with N-SUMO, N-6*His labeled tag. The total length of SLC31A1 Protein, Human (Cell-Free, His-SUMO) is 190 a.a., the molecular weight are 40 KDa (monomer), 80 KDa (dimer), whiel dimers are generally formed.
Oleoylethanolamide-d4 is the deuterium labeled Oleoylethanolamide. Oleoylethanolamide is a highaffinity endogenous PPAR-α agonist, which plays an important role in the treatment of obesity and arteriosclerosis.
Cariprazine-d6 is a deuterium labeled Cariprazine. Cariprazine Cariprazine is an antipsychotic agent that exhibits highaffinity for the D3 (Ki of 0.085 nM) and D2 (Ki of 0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (Ki of 2.6 nM)[1].
Clozapine-d8 is the deuterium labeled Clozapine. Clozapine is an antipsychotic used for the research of schizophrenia. Clozapine has highaffinity for a number of neuroreceptors[1][2][3][4].
Cariprazine-d8 is a deuterium labeled Cariprazine. Cariprazine is a novel antipsychotic agent candidate that exhibits highaffinity for the D3 (Ki=0.085 nM) and D2 (Ki=0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (Ki=2.6 nM).
Oleoylethanolamide-d2 is the deuterium labeled Oleoylethanolamide. Oleoylethanolamide is a highaffinity endogenous PPAR-α agonist, which plays an important role in the treatment of obesity and arteriosclerosis.
Clozapine-d4 is the deuterium labeled Clozapine. Clozapine is an antipsychotic used for the research of schizophrenia. Clozapine has highaffinity for a number of neuroreceptors[1][2][3][4][5].
Aztreonam-d6 is deuterium labeled Aztreonam. Aztreonam (SQ-26,776) is a synthetic monocyclic beta-lactam antibiotic, which has a very highaffinity for penicillin-binding protein 3 (PBP-3).
Pioglitazone-d4 is a deuterium labeled Pioglitazone. Pioglitazone (U 72107) is a potent and selective PPARγ agonist with highaffinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 and 0.99 μM for human and mouse PPARγ, respectively[1].
Trospium-d8 (chloride) is the deuterium labeled Trospium chloride. Trospium chloride is an orally active, specific and competitive antagonist of muscarinic cholinergic receptors (mAChRs), with antimuscarinic activity. Trospium chloride binds to muscarinic receptors M1, M2 and M3 with highaffinity, but not nicotinic, cholinergic receptors[1][2].
Cabergoline-d6 is deuterium labeled Cabergoline. Cabergoline is an ergot derived-dopamine D2-like receptor agonist that has highaffinity for D2, D3, and 5-HT2B receptors (Ki=0.7, 1.5, and 1.2, respectively).
Cabergoline-d5 is the deuterium labeled Cabergoline. Cabergoline is an ergot derived-dopamine D2-like receptor agonist that has highaffinity for D2, D3, and 5-HT2B receptors (Ki=0.7, 1.5, and 1.2, respectively)[1][2].
Pioglitazone-d4 (alkyl) (U 72107-d4 (alkyl)) is the deuterium labeled Pioglitazone. Pioglitazone (U 72107) is a potent and selective PPARγ agonist with highaffinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 and 0.99 μM for human and mouse PPARγ, respectively[1][2].
Emedastine- 13C,d3 (fumarate) is the 13C- and deuterium labeled Emedastine. Emedastine is an orally active, selective and highaffinity histamine H1 receptor antagonist with a Ki value of 1.3 nM. Emedastine is a benzimidazole derivative with potent antiallergic properties and used for allergic rhinitis, allergic skin diseases and allergic conjunctivitis[1][2][3].
cis-Urocanic acid- 13C3 is the 13C-labeled cis-Urocanic acid. cis-Urocanic acid is a 5-HT2A receptor agonist. cis-Urocanic acid binds to 5-HT receptor with relatively highaffinity (Kd=4.6 nM). cis-Urocanic acid is an immune modulator that induces immunosuppression by binding to the 5-HT2A receptor[1].
Barnidipine-d5 (hydrochloride) is the deuterium labeled Barnidipine hydrochloride. Barnidipine hydrochloride (Mepirodipine hydrochloride) is an L-type calcium antagonist (CaA) with highaffinity for [3H] initrendipine binding sites (Ki=0.21 nmol/l), has selective action against CaA receptors[1].Barnidipine hydrochloride (Mepirodipine hydrochloride) is an antihypertensive agent and acts by the reduction of peripheral vascular resistance secondary to its vasodilatory action[2].
UMI-77-d4 is the deuterium labeled UMI-77. UMI-77 is a selective Mcl-1 inhibitor, which shows high binding affinity to Mcl-1 (IC50=0.31 μM). UMI-77 binds to the BH3 binding groove of Mcl-1 with Ki of 490 nM, showing selectivity over other members of anti-apoptotic Bcl-2 members.
MPP+-d3 (iodide) is deuterium labeled MPP+ (iodide). MPP+ iodide, a toxic metabolite of the neurotoxin MPTP, causes symptom of Parkinson's disease in animal models by selectively destroying dopaminergic neurons in substantia nigra. MPP+ iodide is taken up by the dopamine transporter into dopaminergic neurons where it exerts its neurotoxic action on mitochondria by affecting complex I of the respiratory chain. MPP+ iodide is also a highaffinity substrate for the serotonin transporter (SERT)[1][2].
Barnidipine-d5 is the deuterium-labeled Barnidipine (HY-107322A). Barnidipine-d5 (Mepirodipine) is an L-type calcium antagonist (CaA) with highaffinity for [ 3H] initrendipine binding sites (Ki=0.21 nmol/l), has selective action against CaA receptors . Barnidipine-d5 (Mepirodipine) is an antihypertensive agent and acts by the reduction of peripheral vascular resistance secondary to its vasodilatory action .
Dicyclomine-d4 is the deuterium labeled Dicyclomine[1]. Dicyclomine (Dicycloverine) is a potent and orally active muscarinic cholinergic receptors antagonist. Dicyclomine (Dicycloverine) shows highaffinity for muscarinic M1 receptor subtype (Ki=5.1 nM) and M2 receptor subtype (Ki=54.6 nM) in brush-border membrane and basal plasma membranes, respectively[2]. Dicyclomine is an antispasmodic agent and relieves smooth muscle spasm of the gastrointestinal tract in vivo[3].
Propranolol-d7 is the deuterium labeled Propranolol. Propranolol is a nonselective β-adrenergic receptor (βAR) antagonist, has highaffinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively[1]. Propranolol inhibits [3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM[2]. Propranolol is used for the study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy[3].
Propranolol-d7 (ring-d7) is the deuterium labeled Propranolol hydrochloride. Propranolol hydrochloride is a nonselective β-adrenergic receptor (βAR) antagonist, has highaffinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively[1]. Propranolol hydrochloride inhibits [3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM[2]. Propranolol hydrochloride is used for study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy[3].
Relugolix-d6 is deuterium labeled Relugolix. Relugolix (TAK-385) is a potent, orally active, nonpeptidic gonadotropin-releasing hormone (GnRH) antagonist. Relugolix possesses highaffinity and potent antagonistic activity for human receptor (binding IC50=0.33 nM) and monkey receptor (IC50=0.32 nM) compared with TAK-013 (HY-100209)[1]. Relugolix is used for the study of sex-hormone-dependent diseases, such as including endometriosis, uterine fibroids and prostate cancer et al[2].
Olanzapine-d3 is the deuterium labeled Olanzapine. Olanzapine is a selective, orally active monoaminergic antagonist with highaffinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptors (Ki=19 nM). Olanzapine is an atypical antipsychotic[1][2].
Quetiapine-d8 (fumarate) is the deuterium labeled Quetiapine. Quetiapine is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine has moderate to highaffinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects[1][2].
Quetiapine-d8 (hemifumarate) is the deuterium labeled Quetiapine hemifumarate. Quetiapine hemifumarate is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine hemifumarate is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine hemifumarate has moderate to highaffinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects[1].
Quetiapine (hemifumarate)-d8 is the deuterium labeled Quetiapine hemifumarate[1]. Quetiapine hemifumarate is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine hemifumarate is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine hemifumarate has moderate to highaffinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects[2].
Silodosin-d4 is the deuterium labeled Silodosin. Silodosin (KAD 3213) is a potent, selective and orally active α1A-adrenergic receptor (α1A-AR) blocker. Silodosin exhibits highaffinity for α1A-AR (Ki=0.036 nM), over 162-fold and 50-fold than for α1B-AR and α1D-AR with Ki values of 21 nM and 2.0 nM, respectively. Silodosin is an effective and well-tolerated agent, it can be used for the investigation of LUTS/BPH[1][3].
Frovatriptan-d3 (succinate) is deuterium labeled Frovatriptan (succinate). Frovatriptan succinate ((R)-Frovatriptan succinate) is a potent, highaffinity, selective and orally active 5-HT1B (pK50 of 8.2) and 5-HT1D receptor agonist. Frovatriptan succinate exhibits >10-fold selectivity for 5-HT1B and 5-HT1D over 5-HT1A, 5-HT1F, and 5-HT7 and >1000-fold selectivity over other 5-HT, dopamine, histamine H1, and α1-adrenoceptor. Frovatriptan succinate has the potential for migraine research[1][2].
Human, Mouse(predicted: Rat, Dog, Pig, Cow, Horse, Rabbit, Guinea Pig)
CXCR2 Antibody is an unconjugated, approximately 41 kDa, rabbit-derived, anti-CXCR2 polyclonal antibody. CXCR2 Antibody can be used for: WB, ELISA expriments in human, mouse, and predicted: rat, dog, pig, cow, horse, rabbit, guinea pig background without labeling.
Tri-GalNAc-DBCO can bind to the desialic acid glycoprotein receptor (ASGPR) to drive protein downregulation and target protein degradation, where GalNAc is a high-affinity ligand for hepatocyte-specific ASGPR . Tri-GalNAc-DBCO is a click chemistry reagent, it contains a DBCO group that can undergo strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing Azide groups.
EC359 is a potent, selective, highaffinity and orally active leukemia inhibitory factor receptor (LIFR) inhibitor with a Kd of 10.2 nM, which directly interacts with LIFR to effectively block LIF/LIFR interactions . EC359 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Targapremir-210 (TGP-210) is a potent and selective miR-210 (miRNA-210, microRNA-210) inhibitor. Targapremir-210 inhibits pre-miR-210 processing with high binding affinity (Kd~200 nM) . Targapremir-210 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
4-Azidophlorizin is a highaffinityprobe and photoaffinity label for the glucose transporter in brush border membranes . 4-Azidophlorizin is a click chemistry reagent, itcontains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.
TCO-GK-PEG4-NHS ester is an ADC Linker, and can be used for synthesis of [18F]AlF-NOTA-Tz-TCO-GK-2Rs15d. [18F]AlF-NOTA-Tz-TCO-GK-2Rs15d binds with highaffinity and immunoreactivity to HER2 . TCO-GK-PEG4-NHS ester is a click chemistry reagent, it contains a TCO group that can undergo an inverse electron demand Diels-Alder reaction (iEDDA) with molecules containing Tetrazine groups.
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