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Desmethyl cariprazine is a major active metabolite of cariprazine, with activities at human dopamine receptors and serotonin receptors, showing a pEC50 of 8.90 at humanD2receptors, a pEC50 of 8.09 at D3receptors, and a pEC50 of 6.28 at 5-HT1Areceptors. Desmethyl cariprazine inhibits forskolin-induced cAMP production at D2, D3 and 5-HT1Areceptors, and suppresses serotonin-induced Ca 2+ release at 5-HT2Breceptors. Desmethyl cariprazine is applicable to research related to schizophrenia, bipolar disorder type I and bipolar disorder.
Amisulpride ((Rac)-Aramisulpride) is a racemic (50:50) mixture of the R-Amisulpride (HY-109167) and S-Amisulpride (HY-126068). Amisulpride is a dopamine D2/D3receptor antagonist with Ki values of 2.8 and 3.2 nM for human dopamine b>D2 and b>D3, respectively. Amisulpride is a 5-HT7receptor antagonist with a Ki of 44 nM. Amisulpride can be used in psychiatric research .
Melatonin-d3 is the deuterium labeled Melatonin. Melatonin is a hormone made by the pineal gland that can activates melatonin receptor. Melatonin plays a role in sleep and possesses important antioxidative and anti-inflammatory properties . Melatonin is a novel selective ATF-6 inhibitor and induces human hepatoma cell apoptosis through COX-2 downregulation . Melatonin attenuates palmitic acid-induced (HY-N0830) mouse granulosa cells apoptosis via endoplasmic reticulum stress .
Ramelteon metabolite M-II-d3 is the deuterium labeled Ramelteon metabolite M-II. Ramelteon metabolite M-II is the major metabolite of Ramelteon, with IC50s of 208 pM, 1470 pM for human melatonin receptors (MT1 or MT2). Ramelteon is a selective melatonin agonist .
OM-7D3-B3 is an antibody-based antiviral agent targeting the tight junction protein CLDN1 (Kd=4 nM). By binding to the first extracellular domain of CLDN1, OM-7D3-B3 disrupts the formation of the CLDN1-CD81 co-receptor complex, thereby effectively inhibiting the entry of hepatitis C virus (HCV). OM-7D3-B3 not only prevents de novo and chronic HCV infections in humanized liver chimeric mice and uPA-SCID mice transplanted with human livers, but also exhibits favorable safety with no toxic effects observed. OM-7D3-B3 serves as a critical tool for research on HCV infection mechanisms and antiviral drug development .
(+)-PD 128907 hydrochloride is a selective dopamine D2/D3receptor agonist, with Kis of 1.7, 0.84 nM for human and rat D3receptors, 179, 770 n M for human and rat D3receptors, respectively.
GR 103691 is a potent, selective dopamine D3receptor antagonist with a Ki value of 0.4 nM. GR 103691 shows more than 100-fold selectivity for human dopamine human(h)D3 over hD4 and hD1 sites .
Didesmethyl cariprazine is an orally active, BBB-permeable metabolite of Cariprazine (HY-14763). Didesmethyl cariprazine is a partial agonist at the D2 and D3receptors, full agonist at the 5-HT1Areceptor, and antagonist at the human5-HT2Breceptor (Ki: 1.41 nM (human D2L), 0.056 nM (humanD3), 1.7 nM (human 5-HT1A), 0.52 nM (human 5-HT2B)). Didesmethyl cariprazine dose-dependently inhibits the spontaneous activity of rat midbrain dopaminergic neurons .
SB-277011 hydrochloride (SB-277011A hydrochloride) is a potent, selective, orally bioavailable and brain penetrate dopamine D3receptor(D3R) antagonist with Ki values of 10.7 nM and 11.2 nM at rodent and humanD3R, respectively. SB-277011 hydrochloride displays 80- to 100-fold selectivity over other dopamine receptors with pKis of 8.0, 6.0, <5.2, and 5.9 for D3, D2, 5-HT1B, and 5-HT1Dreceptors, respectively .
Amisulpride-d5 is the deuterium labeled Amisulpride. Amisulpride is a dopamine D2/D3receptor antagonist with Kis of 2.8 and 3.2 nM for human dopamine D2 and D3, respectively .
A-381393 is a potent, selective, brain penetrate dopamine D4receptor antagonist, with Kis of 1.5, 1.9 and 1.6 nM for human dopamine D4.4, D4.2, and D4.7receptor, respectively, >2700-fold selectivity over D1, D2, D3 and D5 dopamine receptors. A-381393 shows moderate affinity for 5-HT2A (Ki, 370 nM) .
11-Ketodihydrotestosterone-d3 is the deuterium labeled 11-Ketodihydrotestosterone. 11-Ketodihydrotestosterone (11-KDHT; 5α-Dihydro-11-keto testosterone) is an endogenous steroid and a metabolite of 11β-Hydroxyandrostenedione. 11-Ketodihydrotestosterone is an active androgen and is also a potent androgen receptor (AR) agonist with a Ki of 20.4 nM and an EC50 of 1.35 nM for human AR. 11-Ketodihydrotestosterone drives gene regulation, protein expression and cell growth in androgen-dependent prostate cancer cells .
ABT-724 trihydrochloride is a potent and highly selective dopamine D4receptor agonist with an EC50 of 12.4 nM for human dopamine D4receptor. ABT-724 trihydrochloride is a potent partial agonist at the rat D4 (EC50 of 14.3 nM) and the ferret D4receptor (EC50 of 23.2 nM), and has no effect on dopamine D1, D2, D3, or D5receptors. ABT-724 trihydrochloride could be useful for the treatment of erectile dysfunction and has favorable side-effect profile .
Amitriptyline-d3 hydrochloride is the deuterium labeled Amitriptyline (hydrochloride). Amitriptyline hydrochloride is an inhibitor of serotonin reuptake transporter (SERT) and noradrenaline reuptake transporter (NET), with Kis of 3.45 nM and 13.3 nM for human SERT and NET, respectively. Amitriptyline hydrochloride also weakly binds to dopamine reuptake transporter (DAT) with a Ki of 2.58 μM. Amitriptyline hydrochloride also inhibits adrenergic, muscarinic, histamine and 5-HT receptors. Amitriptyline hydrochloride is a TrkA and TrkBreceptors agonist with potent neurotrophic activity. Amitriptyline hydrochloride has antidepressant activity .
Raxlaprazine etomoxil is a small molecule compound with dopamine D2 and D3receptor modulating activity, which has potential application value in research related to mental illnesses. Raxlaprazine etomoxil exhibits high affinity for human recombinant D2Lreceptors, with an inhibition constant (Ki) of 1.95 nM. Raxlaprazine etomoxil effectively inhibits forskolin-stimulated cAMP accumulation, with an half maximal effective concentration (EC50) of 3.72 nM in functional activity experiments .
ABT-724, a chemical probe, is a potent and highly selective dopamine D4receptor agonist with an EC50 of 12.4 nM for human dopamine D4receptor. ABT-724 is a potent partial agonist at the rat D4 (EC50 of 14.3 nM) and the ferret D4receptor (EC50 of 23.2 nM). ABT-724 has no effect on dopamine D1, D2, D3, or D5receptors. ABT-724 could be useful for the treatment of erectile dysfunction and has favorable side-effect profile .
Agomelatine-d3 is the deuterium labeled Agomelatine. Agomelatine (S-20098) is a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively . Agomelatine is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively .
Mesdopetam (IRL790) is a dopamine D3receptor antagonist (Ki=90 nM; IC50=9.8 μM for human recombinant D3receptor) with psychomotor stabilizing properties. Mesdopetam is used for the research of motor and psychiatric complications in Parkinson disease .
Medroxyprogesterone-d3 is the deuterium labeled Medroxyprogesterone. Medroxyprogesterone is a progestin, a synthetic variant of the human hormone progesterone and a potent progesterone receptor agonist.
Matrine-d3(Matridin-d3) is a deuterium labeled Matrine (HY-N0164). Matrine (Matridin-15-one) is an alkaloid found in plants from the Sophora genus that can act as a kappa opioid receptor and u-receptor agonist. Matrine has a variety of pharmacological effects, including anti-cancer, anti-oxidative stress, anti-inflammation and anti-apoptosis effects. Matrine is potential in the research of disease like human non-small cell lung cancer, hepatoma, papillary thyroid cancer and acute kidney injury (AKI) .
Megestrol acetate-d3 is the deuterium labeled Megestrol acetate. Megestrol acetate is a synthetic and orally active progesteronal agent. Megestrol acetate is effective as an appetite stimulant for wasting syndromes such as cachexia. Megestrol acetate decreases nuclear and cytosol androgen receptorshuman BPH tissue. Megestrol acetate has the potential for HIV study and downregulates autophagic catabolic pathway .
Amisulpride (Standard) is the analytical standard of Amisulpride. This product is intended for research and analytical applications. Amisulpride is a dopamine D2/D3receptor antagonist with Kis of 2.8 and 3.2 nM for humandopamine D2 and D3, respectively.
Amisulpride-d5 N-Oxide is the deuterium labeled Amisulpride. Amisulpride is a dopamine D2/D3receptor antagonist with Kis of 2.8 and 3.2 nM for human dopamine D2 and D3, respectively .
Mesdopetam (IRL790) hemitartrate is a dopamine D3receptor antagonist (Ki=90 nM; IC50=9.8 μM for human recombinant D3receptor) with psychomotor stabilizing properties. Mesdopetam hemitartrate is used for the research of motor and psychiatric complications in Parkinson disease .
RGH-1756 is an atypical antipsychotic that has a strong and selective antagonist activity on humanD3 and less pronounced activity on humanD2L and 5HT1Areceptors .
RG-15 is the orally active antagonist for dopamine receptor that exhibits goof affinity to humanD2 receptor and humanD3receptor with pKi of 8.23 and 10.49. RG-15 inhibits dopamine-stimulated [ 35S]GTPγS binding with IC50 of 21.2 nM (rat striatal membranes), 36.7 nM (mouse A9 cells expressing human D2L receptors) and 7.2 nM (CHO cells expressing humanD3receptors). RG-15 increases the turnover and biosynthesis of dopamine in mouse striatum and olfactory bulb, exhibiting antipsychotic activity .
Elagolix- 13C,d3 (sodium) is the 13C- and deuterium labeled Elagolix sodium. Elagolix sodium is a human GnRH receptor (GnRHR) antagonist with an IC50 and Ki of 0.25 and 3.7 nM, respectively.
Yangonin-d3 is the deuterium labeled Yangonin (HY-N0919). Yangonin exhibits affinity for the human recombinant cannabinoid CB1 receptor with an IC50 and a Ki of 1.79 μM and 0.72 μM, respectively.
N-Despropyl Ropinirole (SKF-104557) is an active metabolite of the dopamine D2 receptor agonist Ropinirole (HY-B0623). N-Despropyl Ropinirole is a full agonist at humanD2 and D3receptors. N-Despropyl Ropinirole is a partial agonistof the hD4 receptor .
Eprosartan-d3 is the deuterium labeled Eprosartan. Eprosartan (SKF-108566J free base) is a selective, competitive, nonpeptid and orally active angiotensin II receptor antagonist, used as an antihypertensive. Eprosartan binds angiotensin II receptor with IC50s of 9.2 nM and 3.9 nM in rat and human adrenal cortical membranes, respectively .
Ercalcitriol-d3 (1α,25-Dihydroxy Vitamin D2-d3) is the deuterium labeled Ercalcitriol (HY-32350). Ercalcitriol (1α,25-Dihydroxy Vitamin D2) is a vitamin D receptor (VDR) agonist with high binding affinity. After binding to VDR, Ercalcitriol forms a complex with retinoid X receptor (RXR) to regulate target gene transcription. For example, Ercalcitriol induces human gingival/oral epithelial cells to produce human cat antimicrobial peptide (hCAP-18/LL-37), which has antimicrobial activity against periodontal pathogens such as Porphyromonas gingivalis. Ercalcitriol enhances the innate immune defense of the oral mucosa by promoting the expression of antimicrobial peptides, and is mainly used in the study of periodontal diseases and immune-related oral diseases .
Megestrol acetate-d3-1 is deuterium labeled Megestrol acetate. Megestrol acetate is a synthetic and orally active progesteronal agent. Megestrol acetate is effective as an appetite stimulant for wasting syndromes such as cachexia. Megestrol acetate decreases nuclear and cytosol androgen receptorshuman BPH tissue. Megestrol acetate has the potential for HIV study and downregulates autophagic catabolic pathway .
PD-143188 (CI 1007) is a selective agonist targeting dopamine (DA) receptors, with Ki values of 25.5 nM and 16.6 nM for human D2 and D3receptors, respectively and lower affinity for D4.2 receptors (Ki=90.9 nM). PD-143188 inhibits DA release, synthesis and metabolism, while reducing cellular cyclic AMP levels, exerting antipsychotic activity. PD-143188 is promising for research of psychopharmacology .
MRS4719-d3 is the deuterium labeled MRS4719 (HY-151547). MRS4719 is a potent P2X4 receptor antagonist with an IC50 value of 0.503 μM for human P2X4 receptor. MRS4719 can reduce infarct volume and reduce brain atrophy, showing neuroprotective and neuro-rehabilitative activities in ischemic stroke model. MRS4719 also reduces ATP-induced [Ca 2+]i influx in primary human monocyte-derived macrophages. MRS4719 can be used to research ischemic stroke .
Benztropine-d3 (mesylate) is the deuterium labeled Benztropine mesylate . Benztropine mesylate (Benzatropine mesylate) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects .
Sarizotan (Standard) is the analytical standard of Sarizotan. This product is intended for research and analytical applications. Sarizotan (EMD 128130) is an orally active serotonin 5-HT1Areceptor and dopamine receptor agonist. Sarizotan (EMD 128130) exhibits IC50 values of 6.5 nM (rat 5-HT1A), 0.1 nM (human 5-HT1A), 15.1 nM (rat D2), 17 nM (human D2), 6.8 nM (humanD3) and 2.4 nM (human D4.2), respectively .
Benztropine- 13C,d3 (mesylate) is the 13C- and deuterium labeled Benztropine (mesylate). Benztropine mesylate (Benzatropine mesylate) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects .
Regadenoson-d3 is the deuterium labeled Regadenoson. Regadenoson (CVT-3146) is a potent and selective A2A adenosine receptor agonist, with Kis of 290 and 1120 nM for rat and pig adenosine A2A receptor, respectively. Regadenoson is selective for the adenosine A2A receptor over adenosine A1 and A2B receptors, and shows 13-fold selectivity over the human adenosine A1 receptor. Regadenoson is a vasodilator stress agent has shifted the landscape of vasodilator myocardial perfusion imaging. Regadenoson increases blood-brain barrier (BBB) permeability in rodents .
Galanthamine-d3 (hydrobromide) is deuterium labeled Galanthamine (hydrobromide). Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC50 of 0.35 μM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD) .
Ganglioside GM2-d3 (ammonium) is the deuterium labeled Ganglioside GM2 (HY-148385). Ganglioside GM2 is a human tumor antigen predominantly found in human tumor cells and fetal brain tissue. As a sialylated glycosphingolipid, Ganglioside GM2 is involved in processes such as cell signaling, adhesion, and motility. Ganglioside GM2 abnormal expression and accumulation are associated with tumors and neurodegenerative disorders. Ganglioside GM2 promotes tumor cell migration and invasion by directly binding to the integrin β1 receptor, activating the FAK/Src/Erk-MAPK signaling pathway, and inducing actin cytoskeleton remodeling .
BMY 28674 (6-Hydroxybuspirone) is the active metabolite of the anxiolytic buspirone (HY-B1115A) and is metabolized by CYP3A4.4. BMY 28674 binds to the serotonin (5-HT) receptor subtype 5-HT1A in the rat hippocampus and dorsal raphe (EC50s are 4 and 1 μM, respectively) and is an antagonist of dopamine D2, D3, and D4 receptors (IC50s are 3.1, 4.9, and 0.85 μM, respectively). BMY 28674 also inhibits organic cation transporter 1 (OCT1), OCT2, and OCT3 expressing human transporters in S2 proximal tubule cells in a concentration-dependent manner.
L 741742 is a highly selective and brain-penetrant D4 dopamine receptor antagonist, with Ki values of 3.5 nM, 770 nM and >1700 nM for human D4, D3 and D2 receptors, respectively. L 741742 suppresses PDGFRβ, ERK1/2, and mTOR signaling pathways, and impairs autophagic flux while disrupting lysosomal function.L 741742 induces G0/G1 cell-cycle arrest and apoptosis, promotes neuronal differentiation of normal human neural stem cells, selectively inhibits growth and clonogenic potential of glioblastoma neural stem cells and primary glioblastoma tumor cells, exerts synergistic effects with Temozolomide (TMZ) (HY-17364) against glioblastoma neural stem cells in vitro, and inhibits glioblastoma neural stem cell xenograft growth in immunocompromised mice. L 741742 can be used for the research of schizophrenia and glioblastoma .
L 741742 hydrochloride is a highly selective and brain-penetrant D4 dopamine receptor antagonist, with Ki values of 3.5 nM, 770 nM and >1700 nM for human D4, D3 and D2 receptors, respectively. L 741742 hydrochloride suppresses PDGFRβ, ERK1/2, and mTOR signaling pathways, and impairs autophagic flux while disrupting lysosomal function.L 741742 hydrochloride induces G0/G1 cell-cycle arrest and apoptosis, promotes neuronal differentiation of normal human neural stem cells, selectively inhibits growth and clonogenic potential of glioblastoma neural stem cells and primary glioblastoma tumor cells, exerts synergistic effects with Temozolomide (TMZ) (HY-17364) against glioblastoma neural stem cells in vitro, and inhibits glioblastoma neural stem cell xenograft growth in immunocompromised mice. L 741742 hydrochloride can be used for the research of schizophrenia and glioblastoma .
Octinoxate-13C,d3 is the deuterium labeled Octinoxate (HY-W245806). Octinoxate (Octyl methoxycinnamate) is a thyroid hormone receptor agonist, reducing the levels of triiodothyronine (T3) and thyroxine (T4) and transcription levels of genes related to type II deiodinase (deio2) in Japanese Medaka. Octinoxate is commonly used as a safe ultraviolet (UV) filter used in the aquatic environment. Octinoxate inhibits CYP1A1 and CYP1B1 to regulate hyaluronan (HA) (HY-B0633A) metabolism in a PI3K pathway-dependent manner in human keratinocytes. Octinoxate also exhibits an anti-estrogenic and anti-androgenic effect in vitro and in vivo .
2-Ethylhexyl (E)-3-(4-(methoxy-d3)phenyl)acrylate is the deuterium labeled Octinoxate (HY-B1234). Octinoxate (Octyl methoxycinnamate) is a thyroid hormone receptor agonist, reducing the levels of triiodothyronine (T3) and thyroxine (T4) and transcription levels of genes related to type II deiodinase (deio2) in Japanese Medaka. Octinoxate is commonly used as a safe ultraviolet (UV) filter used in the aquatic environment. Octinoxate inhibits CYP1A1 and CYP1B1 to regulate hyaluronan (HA) (HY-B0633A) metabolism in a PI3K pathway-dependent manner in human keratinocytes. Octinoxate also exhibits an anti-estrogenic and anti-androgenic effect in vitro and in vivo .
GR 103691 (Standard) is the analytical standard of GR 103691 (HY-101382). This product is intended for research and analytical applications. GR 103691 is a potent, selective dopamine D3receptor antagonist with a Ki value of 0.4 nM. GR 103691 shows more than 100-fold selectivity for human dopamine human (h)D3 over hD4 and hD1 sites .
Desmethyl cariprazine-d8 is the deuterium labeled Desmethyl cariprazine (HY-100656). Desmethyl cariprazine is a major active metabolite of cariprazine, with activities at human dopamine receptors and serotonin receptors, showing a pEC50 of 8.90 at human D2 receptors, a pEC50 of 8.09 at D3receptors, and a pEC50 of 6.28 at 5-HT1A receptors. Desmethyl cariprazine inhibits forskolin-induced cAMP production at D2, D3 and 5-HT1A receptors, and suppresses serotonin-induced Ca 2+ release at 5-HT2B receptors. Desmethyl cariprazine is applicable to research related to schizophrenia, bipolar disorder type I and bipolar disorder.
Didesmethyl cariprazine-d8 is the deuterium labeled Didesmethyl cariprazine (HY-100658). Didesmethyl cariprazine is an orally active, BBB-permeable metabolite of Cariprazine (HY-14763). Didesmethyl cariprazine is a partial agonist at the D2 and D3receptors, full agonist at the 5-HT1A receptor, and antagonist at the human 5-HT2B receptor (Ki: 1.41 nM (human D2L), 0.056 nM (humanD3), 1.7 nM (human 5-HT1A), 0.52 nM (human 5-HT2B)). Didesmethyl cariprazine dose-dependently inhibits the spontaneous activity of rat midbrain dopaminergic neurons.
SB-277011 hydrochloride (Standard) is the analytical standard of SB-277011 (hydrochloride) (HY-10847B). This product is intended for research and analytical applications. SB-277011 hydrochloride (SB-277011A hydrochloride) is a potent, selective, orally bioavailable and brain penetrate dopamine D3receptor (D3R) antagonist with Ki values of 10.7 nM and 11.2 nM at rodent and humanD3R, respectively. SB-277011 hydrochloride displays 80- to 100-fold selectivity over other dopamine receptors with pKis of 8.0, 6.0, <5.2, and 5.9 for D3, D2, 5-HT1B, and 5-HT1D receptors, respectively .
Didesmethyl cariprazine (Standard) is the analytical standard of Didesmethyl cariprazine (HY-100658). This product is intended for research and analytical applications. Didesmethyl cariprazine is an orally active, BBB-permeable metabolite of Cariprazine (HY-14763). Didesmethyl cariprazine is a partial agonist at the D2 and D3receptors, full agonist at the 5-HT1A receptor, and antagonist at the human 5-HT2B receptor (Ki: 1.41 nM (human D2L), 0.056 nM (humanD3), 1.7 nM (human 5-HT1A), 0.52 nM (human 5-HT2B)). Didesmethyl cariprazine dose-dependently inhibits the spontaneous activity of rat midbrain dopaminergic neurons .
L-741626 (Standard) is the analytical standard of L-741626. This product is intended for research and analytical applications. L-741626 is a selective D2 dopamine receptor antagonist, with the Ki values of 2.4, 100 and 220 nM for human D2, D3 and D4 receptors respectively .
SV 293 is a selective antagonist with neutral antagonist activity. SV 293 binds to human D2 receptors with 100-fold higher affinity and has lower affinity for humanD3 and D4 dopamine receptor subtypes. SV 293 was found to block the effects of the full agonist quinpirole in forskolin-dependent adenylate acylase inhibition assays and electrophysiological assays. SV 293 can be used as a useful pharmacological tool to study the role of dopamine D2-like receptor subtypes in dopamine pathways associated with neurological, neuropsychiatric and movement disorders .
ABT-724 trihydrochloride (Standard) is the analytical standard of ABT-724 trihydrochloride (HY-103409). This product is intended for research and analytical applications. ABT-724 trihydrochloride is a potent and highly selective dopamine D4 receptor agonist with an EC50 of 12.4 nM for human dopamine D4 receptor. ABT-724 trihydrochloride is a potent partial agonist at the rat D4 (EC50 of 14.3 nM) and the ferret D4 receptor (EC50 of 23.2 nM), and has no effect on dopamine D1, D2, D3, or D5 receptors. ABT-724 trihydrochloride could be useful for the treatment of erectile dysfunction and has favorable side-effect profile .
Dopamine D3 receptor agonist-2 is a selective dopamineD3 receptor partial agonist with a Ki of 0.268 nM. Dopamine D3 receptor agonist-2 exhibits 29-fold selectivity over dopamineD2 receptor (Ki= 7.67nM) .
OM-7D3-B3 is an antibody-based antiviral agent targeting the tight junction protein CLDN1 (Kd=4 nM). By binding to the first extracellular domain of CLDN1, OM-7D3-B3 disrupts the formation of the CLDN1-CD81 co-receptor complex, thereby effectively inhibiting the entry of hepatitis C virus (HCV). OM-7D3-B3 not only prevents de novo and chronic HCV infections in humanized liver chimeric mice and uPA-SCID mice transplanted with human livers, but also exhibits favorable safety with no toxic effects observed. OM-7D3-B3 serves as a critical tool for research on HCV infection mechanisms and antiviral drug development .
Vitamin D receptor (VDR) acts as a nuclear receptor for calcitriol, the active form of vitamin D3, triggering cellular effects. After vitamin D3 binding, VDR translocates to the nucleus and forms a heterodimer with the retinoid X receptor (RXR). Vitamin D Receptor/VDR Protein, Human (sf9, His) is the recombinant human-derived Vitamin D Receptor/VDR protein, expressed by Sf9 insect cells , with C-10*His labeled tag.
Melatonin-d3 is the deuterium labeled Melatonin. Melatonin is a hormone made by the pineal gland that can activates melatonin receptor. Melatonin plays a role in sleep and possesses important antioxidative and anti-inflammatory properties . Melatonin is a novel selective ATF-6 inhibitor and induces human hepatoma cell apoptosis through COX-2 downregulation . Melatonin attenuates palmitic acid-induced (HY-N0830) mouse granulosa cells apoptosis via endoplasmic reticulum stress .
Ramelteon metabolite M-II-d3 is the deuterium labeled Ramelteon metabolite M-II. Ramelteon metabolite M-II is the major metabolite of Ramelteon, with IC50s of 208 pM, 1470 pM for human melatonin receptors (MT1 or MT2). Ramelteon is a selective melatonin agonist .
Amisulpride-d5 is the deuterium labeled Amisulpride. Amisulpride is a dopamine D2/D3receptor antagonist with Kis of 2.8 and 3.2 nM for human dopamine D2 and D3, respectively .
11-Ketodihydrotestosterone-d3 is the deuterium labeled 11-Ketodihydrotestosterone. 11-Ketodihydrotestosterone (11-KDHT; 5α-Dihydro-11-keto testosterone) is an endogenous steroid and a metabolite of 11β-Hydroxyandrostenedione. 11-Ketodihydrotestosterone is an active androgen and is also a potent androgen receptor (AR) agonist with a Ki of 20.4 nM and an EC50 of 1.35 nM for human AR. 11-Ketodihydrotestosterone drives gene regulation, protein expression and cell growth in androgen-dependent prostate cancer cells .
Agomelatine-d3 is the deuterium labeled Agomelatine. Agomelatine (S-20098) is a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively . Agomelatine is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively .
Medroxyprogesterone-d3 is the deuterium labeled Medroxyprogesterone. Medroxyprogesterone is a progestin, a synthetic variant of the human hormone progesterone and a potent progesterone receptor agonist.
Matrine-d3(Matridin-d3) is a deuterium labeled Matrine (HY-N0164). Matrine (Matridin-15-one) is an alkaloid found in plants from the Sophora genus that can act as a kappa opioid receptor and u-receptor agonist. Matrine has a variety of pharmacological effects, including anti-cancer, anti-oxidative stress, anti-inflammation and anti-apoptosis effects. Matrine is potential in the research of disease like human non-small cell lung cancer, hepatoma, papillary thyroid cancer and acute kidney injury (AKI) .
Megestrol acetate-d3 is the deuterium labeled Megestrol acetate. Megestrol acetate is a synthetic and orally active progesteronal agent. Megestrol acetate is effective as an appetite stimulant for wasting syndromes such as cachexia. Megestrol acetate decreases nuclear and cytosol androgen receptorshuman BPH tissue. Megestrol acetate has the potential for HIV study and downregulates autophagic catabolic pathway .
Amisulpride-d5 N-Oxide is the deuterium labeled Amisulpride. Amisulpride is a dopamine D2/D3receptor antagonist with Kis of 2.8 and 3.2 nM for human dopamine D2 and D3, respectively .
Elagolix- 13C,d3 (sodium) is the 13C- and deuterium labeled Elagolix sodium. Elagolix sodium is a human GnRH receptor (GnRHR) antagonist with an IC50 and Ki of 0.25 and 3.7 nM, respectively.
Yangonin-d3 is the deuterium labeled Yangonin (HY-N0919). Yangonin exhibits affinity for the human recombinant cannabinoid CB1 receptor with an IC50 and a Ki of 1.79 μM and 0.72 μM, respectively.
Eprosartan-d3 is the deuterium labeled Eprosartan. Eprosartan (SKF-108566J free base) is a selective, competitive, nonpeptid and orally active angiotensin II receptor antagonist, used as an antihypertensive. Eprosartan binds angiotensin II receptor with IC50s of 9.2 nM and 3.9 nM in rat and human adrenal cortical membranes, respectively .
Ercalcitriol-d3 (1α,25-Dihydroxy Vitamin D2-d3) is the deuterium labeled Ercalcitriol (HY-32350). Ercalcitriol (1α,25-Dihydroxy Vitamin D2) is a vitamin D receptor (VDR) agonist with high binding affinity. After binding to VDR, Ercalcitriol forms a complex with retinoid X receptor (RXR) to regulate target gene transcription. For example, Ercalcitriol induces human gingival/oral epithelial cells to produce human cat antimicrobial peptide (hCAP-18/LL-37), which has antimicrobial activity against periodontal pathogens such as Porphyromonas gingivalis. Ercalcitriol enhances the innate immune defense of the oral mucosa by promoting the expression of antimicrobial peptides, and is mainly used in the study of periodontal diseases and immune-related oral diseases .
Megestrol acetate-d3-1 is deuterium labeled Megestrol acetate. Megestrol acetate is a synthetic and orally active progesteronal agent. Megestrol acetate is effective as an appetite stimulant for wasting syndromes such as cachexia. Megestrol acetate decreases nuclear and cytosol androgen receptorshuman BPH tissue. Megestrol acetate has the potential for HIV study and downregulates autophagic catabolic pathway .
MRS4719-d3 is the deuterium labeled MRS4719 (HY-151547). MRS4719 is a potent P2X4 receptor antagonist with an IC50 value of 0.503 μM for human P2X4 receptor. MRS4719 can reduce infarct volume and reduce brain atrophy, showing neuroprotective and neuro-rehabilitative activities in ischemic stroke model. MRS4719 also reduces ATP-induced [Ca 2+]i influx in primary human monocyte-derived macrophages. MRS4719 can be used to research ischemic stroke .
Benztropine-d3 (mesylate) is the deuterium labeled Benztropine mesylate . Benztropine mesylate (Benzatropine mesylate) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects .
Benztropine- 13C,d3 (mesylate) is the 13C- and deuterium labeled Benztropine (mesylate). Benztropine mesylate (Benzatropine mesylate) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects .
Regadenoson-d3 is the deuterium labeled Regadenoson. Regadenoson (CVT-3146) is a potent and selective A2A adenosine receptor agonist, with Kis of 290 and 1120 nM for rat and pig adenosine A2A receptor, respectively. Regadenoson is selective for the adenosine A2A receptor over adenosine A1 and A2B receptors, and shows 13-fold selectivity over the human adenosine A1 receptor. Regadenoson is a vasodilator stress agent has shifted the landscape of vasodilator myocardial perfusion imaging. Regadenoson increases blood-brain barrier (BBB) permeability in rodents .
Galanthamine-d3 (hydrobromide) is deuterium labeled Galanthamine (hydrobromide). Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC50 of 0.35 μM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD) .
Ganglioside GM2-d3 (ammonium) is the deuterium labeled Ganglioside GM2 (HY-148385). Ganglioside GM2 is a human tumor antigen predominantly found in human tumor cells and fetal brain tissue. As a sialylated glycosphingolipid, Ganglioside GM2 is involved in processes such as cell signaling, adhesion, and motility. Ganglioside GM2 abnormal expression and accumulation are associated with tumors and neurodegenerative disorders. Ganglioside GM2 promotes tumor cell migration and invasion by directly binding to the integrin β1 receptor, activating the FAK/Src/Erk-MAPK signaling pathway, and inducing actin cytoskeleton remodeling .
Octinoxate-13C,d3 is the deuterium labeled Octinoxate (HY-W245806). Octinoxate (Octyl methoxycinnamate) is a thyroid hormone receptor agonist, reducing the levels of triiodothyronine (T3) and thyroxine (T4) and transcription levels of genes related to type II deiodinase (deio2) in Japanese Medaka. Octinoxate is commonly used as a safe ultraviolet (UV) filter used in the aquatic environment. Octinoxate inhibits CYP1A1 and CYP1B1 to regulate hyaluronan (HA) (HY-B0633A) metabolism in a PI3K pathway-dependent manner in human keratinocytes. Octinoxate also exhibits an anti-estrogenic and anti-androgenic effect in vitro and in vivo .
2-Ethylhexyl (E)-3-(4-(methoxy-d3)phenyl)acrylate is the deuterium labeled Octinoxate (HY-B1234). Octinoxate (Octyl methoxycinnamate) is a thyroid hormone receptor agonist, reducing the levels of triiodothyronine (T3) and thyroxine (T4) and transcription levels of genes related to type II deiodinase (deio2) in Japanese Medaka. Octinoxate is commonly used as a safe ultraviolet (UV) filter used in the aquatic environment. Octinoxate inhibits CYP1A1 and CYP1B1 to regulate hyaluronan (HA) (HY-B0633A) metabolism in a PI3K pathway-dependent manner in human keratinocytes. Octinoxate also exhibits an anti-estrogenic and anti-androgenic effect in vitro and in vivo .
Desmethyl cariprazine-d8 is the deuterium labeled Desmethyl cariprazine (HY-100656). Desmethyl cariprazine is a major active metabolite of cariprazine, with activities at human dopamine receptors and serotonin receptors, showing a pEC50 of 8.90 at human D2 receptors, a pEC50 of 8.09 at D3receptors, and a pEC50 of 6.28 at 5-HT1A receptors. Desmethyl cariprazine inhibits forskolin-induced cAMP production at D2, D3 and 5-HT1A receptors, and suppresses serotonin-induced Ca 2+ release at 5-HT2B receptors. Desmethyl cariprazine is applicable to research related to schizophrenia, bipolar disorder type I and bipolar disorder.
Didesmethyl cariprazine-d8 is the deuterium labeled Didesmethyl cariprazine (HY-100658). Didesmethyl cariprazine is an orally active, BBB-permeable metabolite of Cariprazine (HY-14763). Didesmethyl cariprazine is a partial agonist at the D2 and D3receptors, full agonist at the 5-HT1A receptor, and antagonist at the human 5-HT2B receptor (Ki: 1.41 nM (human D2L), 0.056 nM (humanD3), 1.7 nM (human 5-HT1A), 0.52 nM (human 5-HT2B)). Didesmethyl cariprazine dose-dependently inhibits the spontaneous activity of rat midbrain dopaminergic neurons.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
MedchemExpress Validation 03
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
MedchemExpress Validation 04
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
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