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Muvalaplin (LY3473329) is an orally active, selective small molecule inhibitor of lipoprotein (a) (Lp (a)) that disrupts the initial non-covalent interaction between apo(a) and apoB100, preventing the disulphide bond and Lp(a)
formation. Muvalaplin reduces the levels of Lp (a) in transgenic mice and in cynomolgus monkeys .
Maridebart cafraglutide (AMG 133) is a long-acting peptide-antibody conjugate that combines GLP-1 receptor agonist with glucose-dependent insulinotropic polypeptide (GIP) receptor antagonism. Maridebart cafraglutide shows antagonist activity against human, cynomolgus monkey and rat GIPR with IC50 values of 46.4 nM, 26.5 nM, 822.3 nM, respectively. Maridebart cafraglutide shows agonist activity against human, cynomolgus monkey, rat and mouse GLP-1R with EC50 values of 24.4 pM, 5.7 pM, 2.4 pM and 123 pM, respectively. Maridebart cafraglutide can be used for the study of obesity and type 2 diabetes .
GSK2982772 is a potent, orally active and ATP competitive RIP1 kinase inhibitor with IC50 values of 16 nM and 20 nM for human and monkey RIP1, respectively .
Dersimelagon (MT-7117) is an orally active, selective melanocortin 1 receptor (MC1R) agonist with EC50 values of 8.16, 3.91, 1.14 and 0.251 nM for human (h), cynomolgus monkey (cm), mouse (m) and rat (r) MC1R, respectively. Dersimelagon shows good affinity for hMC1R and hMC4R with Ki values of 2.26, 32.9 nM, respectively. Dersimelagon can be used for the research of skin pigmentation .
ATR-107 (PF-05230900) is a humanized monoclonal antibody inhibitor that targets the interleukin-21 receptor (IL-21R). The Ka value of ATR-107 is 2-4 nM in cynomolgus monkeys, 16 nM in mice, and 71 nM in rats. ATR-107 can be used in research related to systemic lupus erythematosus and air pouch inflammation .
Raludotatug Deruxtecan is an antibody-drug conjugate targeting CDH6, with an EC50 of 64.7 ng/mL in humans, 70.4 ng/mL in cynomolgus monkeys, and 228 ng/mL in mice. Raludotatug Deruxtecan specifically binds to CDH6 on the surface of cancer cells, triggers lysosomal internalization, and releases the DXd payload that inhibits TOP1. Raludotatug Deruxtecan induces DNA damage, Chk1 phosphorylation, caspase-3 cleavage, apoptosis, and bystander cell death. Raludotatug Deruxtecan is applicable to research related to serous ovarian cancer and renal cell carcinoma .
Erenumab (AMG-334) is a fully human monoclonal antibody. Erenumab inhibits the calcitonin gene-related peptide (CGRP) receptor. Erenumab prevents the increase in dermal blood flow in cynomolgus monkeys. Erenumab can be used in the research of episodic migraine .
Vicadrostat (BI 690517) is an orally active aldosterone synthase (aldosterone synthase) inhibitor, with IC50 values of 19 nM, 16 nM, and 18 μM against human, cynomolgus monkey, and rat aldosterone synthase, respectively. Vicadrostat has an in vivo IC50 of 25 nM for aldosterone synthesis. Vicadrostat exhibits high selectivity for cortisol synthase; it reduces aldosterone production and decreases plasma aldosterone levels. Vicadrostat can be used in the research of chronic kidney disease, heart failure, and hypertension .
Melredableukin alfa (RG7835) is a bivalent conjugate composed of a human IL-2 mutant (T3A, N88D, C125A) and human IgG1. Melredableukin alfa exhibits enhanced Treg cell selectivity in cynomolgus monkey and humanized mouse models. Melredableukin alfa can be used in research related to ulcerative colitis and autoimmune hepatitis .
Rondaptivon pegol (BT200) sodium is an aptamer targeting von Willebrand factor (VWF), with an EC50 of 33 nM in humans. Rondaptivon pegol sodium effectively alleviates acute myocardial ischemia-reperfusion injury in mice by inhibiting VWF activity, reducing microvascular obstruction, inflammatory responses and cardiomyocyte apoptosis (apoptosis). Rondaptivon pegol sodium inhibits the binding of VWF to platelet glycoprotein GPIb, thereby preventing arterial thrombosis in cynomolgus monkeys. Rondaptivon pegol sodium can be used in research related to arterial thrombosis, stroke, myocardial infarction and myocardial ischemia-reperfusion injury .
WIZ degrader 9 is an orally active molecular glue degrader of the WIZ transcription factor. As a molecular glue, WIZ degrader 9 recruits WIZ to the cereblon E3 ubiquitin ligase complex via its ZF7 domain, driving proteasome-dependent degradation of WIZ. WIZ degrader 9 induces hemoglobin production, reduces the level of H3K9 dimethylation across the whole genome and at the β-globin locus, upregulates the transcription of γ-globin and BGLT3, and increases the level of histone H3K9 acetylation in the promoter region of HBG1/2. WIZ degrader 9 effectively induces fetal hemoglobin production in both mice and cynomolgus monkeys. WIZ degrader 9 can be used for research on sickle cell disease .
Hydroxyprogesterone caproate (17α-Hydroxyprogesterone hexanoate; 17α-Hydroxyprogesterone caproate) is a progesterone receptor (progesterone receptor) ligand and steroid hormone transcription inhibitor. Hydroxyprogesterone caproate downregulates estrogen receptors in target tissues and activates their metabolic pathways, and exhibits equivalent affinity for progesterone receptor A and progesterone receptor B. Hydroxyprogesterone caproate shows no consistent teratogenicity or developmental toxicity in rat, mouse and monkey models, but induces resorption or abortion in rhesus monkeys at human-equivalent doses. Hydroxyprogesterone caproate promotes the production of TNF-α in lipopolysaccharide-stimulated whole blood from non-pregnant women. Hydroxyprogesterone caproate can be used in scientific research related to preterm birth .
Cemdisiran (ALN-CC5) is an N-acetylgalactosamine-conjugated RNAi agent and also a complement component C5 inhibitor. Cemdisiran targets C5 mRNA, cleaves C5 mRNA via the endogenous RNA interference pathway, and inhibits the production of C5 protein in the liver. Cemdisiran exerts a dose-dependent inhibitory effect on total C5 concentrations in cynomolgus monkeys. When used in combination with Pozelimab (HY-P99786) in cynomolgus monkeys, Cemdisiran achieves a more sustained and complete inhibitory effect on complement activity. Cemdisiran can be used in the research of paroxysmal nocturnal hemoglobinuria and other complement-mediated diseases .
Flizasertib (GDC-8264) is an orally active, reversible and selective RIP1 inhibitor with Kiapp values of 0.00071 μM and 0.0013 μM for human and cynomolgus monkey RIP1 kinase, respectively. Flizasertib blocks RIP1 autophosphorylation but does not affect RIP1 protein stability. Flizasertib inhibits pro-inflammatory cytokines (CCL3, CCL4, and IL-1β) production. Flizasertib results in inhibition of colitis and ileitis. Flizasertib can be used in the research of cardiac surgery-associated acute kidney injury .
Emugrobart (GYM-329, RG6237, RG-70240) is a humanized IgG1κ antibody targeting myostatin (Myostatin; GDF8). Emugrobart binds to pro-myostatin and latent myostatin, blocking their cleavage into mature myostatin; it also has a clearance function, which transports bound myostatin for degradation and allows for cyclic reuse. Emugrobart enhances muscle strength in mouse models of muscle atrophy and increases muscle mass in cynomolgus monkeys. Emugrobart can be used in research on spinal muscular atrophy and facioscapulohumeral muscular dystrophy .
SNX281 is a selective STING agonist, with IC50 values of 4.1, 4.5, 10.7, and 3.7 μM against human, mouse, rat, and monkey STING, respectively. SNX281 undergoes homodimerization at the STING binding site, triggering a conformational shift of STING from an inactive open state to an active closed state, thereby driving downstream STING-dependent signaling pathways. SNX281 induces type I interferons, IFN-β, TNF-α, IL-6, cytokine release, T cell responses, and long-lasting immune memory. SNX281 exhibits anti-tumor activity and is applicable to research related to colorectal cancer, melanoma, advanced solid tumors, lymphoma, and ovarian cancer .
SAR441255 is a potent unimolecular peptide GLP-1/GIP/GCG receptor triagonist. SAR441255 displays high potency with balanced activation of all three target receptors.?SAR441255 shows positive acute glucoregulatory effectss in diabetic obese monkeys .
Cloprostenol is a prostaglandin F-2α (PGF2α (HY-12956)) analogue. Cloprostenol induces luteolysis in marmoset monkeys. Cloprostenol can be used for the research of open-cervix pyometra .
Quetmolimab (E6011) is a humanized anti-Fractalkine (CX3CL1) monoclonal antibody. Quetmolimab binds to membrane-bound and soluble Fractalkine, neutralizes Fractalkine-induced migration of CX3CR1-expressing cells, mediates target-bound complex elimination from serum. Quetmolimab suppresses free soluble Fractalkine levels in cynomolgus monkeys, with target engagement linked to increased serum total Fractalkine concentration. Quetmolimab can be used for the research of Crohn’s disease, rheumatoid arthritis, and primary biliary cholangitis .
Avosentan (Ro 67-0565; SPP-301) is an orally active endothelin (ETA) receptor antagonist. Avosentan can block the ETA receptor, thereby reducing vascular contraction and exerting a renal protective effect. Avosentan inhibits vascular contraction caused by ET-1 and alleviates the reduction in retinal and optic nerve head blood flow induced by it, lowering intraocular pressure in the glaucoma monkey model. Avosentan non-specifically blocks ETB receptors at high doses, inhibiting ETB-mediated diuresis and natriuresis, and may cause fluid retention. Avosentan can be used to reduce proteinuria with diabetic nephropathy, but induces significant fluid overload and congestive heart failure .
Ruzasvir (MK-8408) is an orally active inhibitor for genotypic HCV nonstructural protein 5A (NS5A), which inhibits the replication of NS5A mutants GT1a, GT1a L31V, GT1a Y93H, GT2b, GT3a and GT4a with EC90 ranging from 0.003 to 0.067 nM. Ruzasvir exhibits good pharmacokinetic characters in rhesus monkey model .
ISIS 104838 is an antisense oligonucleotide targeting TNF-α. ISIS 104838 specifically binds to human TNF-α mRNA via Watson-Crick base pairing to form a DNA:RNA hybrid duplex, thereby recruiting the ubiquitously expressed intracellular enzyme RNase H to degrade the target mRNA and inhibit TNF-α protein synthesis at the transcriptional level. ISIS 104838 induces moderate, self-limiting thrombocytopenia in cynomolgus monkeys. ISIS 104838 can be used for the study of inflammatory diseases .
ABBV-154 is an anti-TNF antibody-drug conjugate (ADC). ABBV-154 is composed of the humanized antibody Adalimumab (HY-P9908) conjugated with a glucocorticoid receptor modulator (HY-137883). ABBV-154 can be used in studies of rheumatoid arthritis, Crohn's disease and polymyalgia rheumatica .
RO5166017 is an orally active and species-crosses TAAR1 agonist, with Ki values of 1.9 nM, 2.7 nM, 31 nM and 24 nM for mouse, rat, human and cynomolgus monkey, respectively .
Pamaquine is an 8-aminoquinoline antimalarial agent. Pamaquine has neurotoxicity and can damage specific neuro-anatomical structures, leading to deficits of neurologic function in Rhesus monkeys models .
Anti-Monkey/Human CD28 Antibody (CD28.2) is a mouse-derived IgG1 κ type antibody inhibitor, targeting to monkey/human CD28. Anti-Monkey/Human CD28 Antibody (CD28.2) can block CD28 signaling. Anti-Monkey/Human CD28 Antibody (CD28.2) can be used for the research of immunology .
Anti-Monkey/Human MHC class II (HLA-DR) Antibody (L243) is a mouse-derived IgG2a κ type antibody inhibitor, targeting to monkey/human MHC class II. Anti-Monkey/Human MHC class II (HLA-DR) Antibody (L243) can inhibits tumor cells proliferation and induce apoptosis. Anti-Monkey/Human MHC class II (HLA-DR) Antibody (L243) increases cellular reactive oxygen species (ROS) and loss of mitochondrial membrane potential in human endothelial cells. Anti-Monkey/Human MHC class II (HLA-DR) Antibody (L243) can be used for the researches of cancer and infection, such as lymphoma .
Anti-Monkey/Human CD40L/CD154 Antibody (5C8) is a mouse-derived IgG2a type antibody inhibitor, targeting to monkey/human CD40L/CD154. Anti-Monkey/Human CD40L/CD154 Antibody (5C8) blocks the interactionbetween CD154 and CD40. Anti-Monkey/Human CD40L/CD154 Antibody (5C8) can be used for the researches of inflammation and immunology, such as colitis and transplant .
Cynomolgus Monkey serum albumin is a plasma protein derived from cynomolgus monkey. Serum albumin is a multifunctional protein with extraordinary ligand binding capacity, making it a transporter molecule for a diverse range of metabolites, drugs, nutrients, metals and other molecules.
Adrogolide hydrochloride (ABT-431 hydrochloride) is a chemically stable prodrug that can convert to the dopamine D1 receptor agonist A-86929. Adrogolide hydrochloride ameliorates the MPTP (HY-15608)-induced Parkinson's Disease in marmoset model, reduces the dyskinesias tendency. Adrogolide hydrochloride reverses Risperidone (HY-11018)-induced cognitive deficits in monkey .
MB-07729 is a potent fructose 1,6-bisphosphatase (FBPase) noncompetitive inhibitor with IC50 values of 31, 121, and 189 nM for human, monkey, and rat, respectively.
BAY-1128688 is a potent, orally active and selective AKR1C3 inhibitor with IC50 < 2 nM. BAY-1128688 shows high selectivity over related AKR1C enzymes (1C1, 1C2, 1C4) and AKR1D1. BAY-1128688 exhibits no relevant activity at major nuclear hormone receptors. BAY-1128688 reduces endometriotic lesions in the marmoset monkey endometriosis model. BAY-1128688 can be used for endometriosis research .
ABT-384 is a potent, selective 11-β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor. ABT-384 exhibits high affinity (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) .
Anti-Monkey/Human MDR-1/CD243 Antibody (UIC2) is an anti-monkey/human MDR-1/CD243 IgG2a monoclonal antibody. Anti-Monkey/Human MDR-1/CD243 Antibody (UIC2) can efficiently inhibit P-glycoprotein. Anti-Monkey/Human MDR-1/CD243 Antibody (UIC2) enhances the inhibitory effect on multidrug resistance (MDR) by suppressing drug efflux. Anti-Monkey/Human MDR-1/CD243 Antibody (UIC2) can be used for research on cancer .
ATP6V1A Monkey Pre-designed siRNA Set A contains three designed siRNAs for ATP6V1A gene (Monkey), as well as a negative control, a positive control, and a FAM-labeled negative control.
NPRA agonist-11 (Example 161) is an NPRA (NPR1) agonist, with AC50 values of 1.681 μM and 0.989 μM for humans and monkeys, respectively. NPRA agonist-11 can be used in the research of cardiovascular diseases and other disorders .
SAR441255 TFA is a potent unimolecular peptide GLP-1/GIP/GCG receptor triagonist. SAR441255 TFA displays high potency with balanced activation of all three target receptors.?SAR441255 TFA shows positive acute glucoregulatory effectss in diabetic obese monkeys .
MDAN-21 is a bivalent opioid ligand that contains both μ-opioid receptor agonists and δ-opioid receptor antagonists. MDAN-21 has a strong analgesic effect and does not produce tolerance in mouse studies. MDAN-21 can effectively inhibit the withdrawal of morphine dependent monkeys and alleviate abnormal pain in the study of rhesus monkeys. MDAN-21 can be used for the study of allodynia .
GSK 1562590 hydrochloride is a high affinity 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 .
Anti-Monkey/Human CD20 Antibody (2H7) is a mouse-derived IgG2b κ type antibody inhibitor, targeting to monkey/human CD20. Anti-Monkey/Human CD20 Antibody (2H7) specifically depletes B cells. Anti-Monkey/Human CD20 Antibody (2H7) can be used for the researches of inflammation and metabolic disease, such as diabetes and experimental autoimmune encephalomyelitis .
Kallikrein, Cynomolgus Monkey is proteolytically cleaves high molecular weight kininogen to generate the potent vasodilator and the pro-inflammatory peptide, bradykinin. can be used for the research of inflammation .
5-Hydroxy saxagliptin hydrochloride is an active metabolite of Saxagliptin (HY-10285) and a potent and selective DPP-4 inhibitor. 5-Hydroxy saxagliptin hydrochloride has Ki values of 2.6 nM and 2.9 nM for humans and cynomolgus monkeys, respectively. 5-Hydroxy saxagliptin hydrochloride can be used in the research of type 2 diabetes mellitus .
Dersimelagon phosphate is an orally active, selective melanocortin 1 receptor (MC1R) agonist with EC50 values of 8.16, 3.91, 1.14 and 0.251 nM for human (h), cynomolgus monkey (cm), mouse (m) and rat (r) MC1R, respectively. Dersimelagon phosphate shows good affinity for hMC1R and hMC4R with Ki values of 2.26, 32.9 nM, respectively. Dersimelagon phosphate can be used for the research of skin pigmentation .
NGD 94-1 (dimaleate) is a potent and selective dopamine D4 receptor antagonist. NGD 94-1 (dimaleate) shows high affinity for the cloned human D4.2 receptor (Ki = 3.6 nM). NGD 94-1 (dimaleate) modulates the cognitive functions of the frontostriatal system and regulates dopaminergic transmission in Phencyclidine (PCP)-induced monkeys. NGD 94-1 (dimaleate) can be used for neurological disease research [1][2].
MK 1256 is a highly selective and orally active inhibitor of tissue protease K (Cat K) with an IC50 of 0.62 nM. MK 1256 shows extremely high selectivity towards other tissue proteases (all > 1100 times), with only a slightly lower selectivity for tissue protease F (Cat F) (110 times). MK 1256 exhibits strong anti-bone resorption activity in the osteoporosis model of rhesus monkeys with ovariectomy. MK 1256 can be used for research on osteoporosis .
BIIB042 is a potent, orally active, brain-penetrant, and selective γ-secretase modulator (GSM). BIIB042 reduces Aβ42 and increases Aβ38 levels in cells. BIIB042 significantly reduces brain Aβ42 levels in CF-1 mice and Fischer rats, as well as plasma Aβ42 levels in cynomolgus monkeys. BIIB042 reduces Aβ42 levels and Aβ plaque burden in Tg2576 mice. BIIB042 can be used for alzheimer's disease (AD) research .
TLR7/8 agonist 13 is an orally active dual agonist of TLR7 (lowest effective concentrations (LEC) [hTLR7] = 1.6 μM) and TLR8 (LEC [hTLR8] = 1.6 μM). TLR7/8 agonist 13 exhibits agonistic activity against human peripheral blood mononuclear cells (hPBMCs) (LEC [hPBMC] = 0.5 μM). TLR7/8 agonist 13 induces endogenous IFNα, activating myeloid dendritic cells and monocytes toward a TH1 phenotype in mice and cynomolgus monkeys. TLR7/8 agonist 13 reduces viral load and HBV surface antigen expression in a mouse model of chronic AAV-HBV infection. TLR7/8 agonist 13 has the potential to indirectly induce IFNγ, which may promote HBV antigen-specific CD8 T cell-mediated responses. TLR7/8 agonist 13 can be used to study hepatitis B virus .
Bentysrepinine (Y101) is an orally active HBV inhibitor with anti-hepatitis B virus infection activity. Bentysrepinine exhibits favorable pharmacokinetic characteristics, with absolute bioavailability of 44.9%, 43.1%, and 19.2% in rats, dogs, and monkeys, respectively, and it does not accumulate in monkeys after 90 days of oral administration. Bentysrepinine is under research in the antiviral and hepatitis fields .
Hyzetimibe is a cholesterol absorption inhibitor. Hyzetimibe blocks the intestinal absorption of cholesterol and phytol. Hyzetimibe is well tolerated in animal models, with an LDmax 2000 mg/kg in rats and an LDmax 500 mg/kg in rhesus monkeys .
Anti-Mouse/Rat/Monkey/Human ICOS/CD278 Antibody (C398.4A) is an anti-mouse/rat/monkey/human ICOS/CD278 IgG monoclonal antibody. Anti-Mouse/Rat/Monkey/Human ICOS/CD278 Antibody (C398.4A) has limited effectiveness in improving T cell function and immune activation. Anti-Mouse/Rat/Monkey/Human ICOS/CD278 Antibody (C398.4A) can be used for researches on cancer and infection conditions such as gliomas and hepatitis B virus infection .
DCCCyB is an orally bioavailable, potent, and selective inhibitor of GlyT1. DCCCyB demonstrates excellent in vivo occupancy of GlyT1 transporters in rhesus monkey .
Tiospirone (MJ 13859-1) hydrochloride is an orally active antipsychotic agent that reduces or eliminates tardive dyskinesia (TD) in Cebus apella monkeys with persistent TD .
DS79932728 is an orally active inhibitor for G9a and GLP with IC50 of 12.6 nM and 75.7 nM. DS79932728 induces the production of γ-globin, thereby increasing the level of fetal hemoglobin (HbF). DS79932728 increases F-reticulocytes (F-rets) proportion and exhibits good oral absorption characteristics in cynomolgus monkey models .
GS-8873 is an orally active inhibitor for the production of hepatitis B virus (HBV) surface antigen (HBsAg) with an EC50 of 4 nM. GS-8873 exhibits good pharmacokinetic characters in rats and metabolic stability in human hepatocytes. GS-8873 causes neurofunctional deficits in rats and cynomolgus monkeys .
NGD94-1 is a potent and selective dopamine D4 receptor antagonist. NGD94-1 shows high affinity for the cloned human D4.2 receptor (Ki = 3.6 nM). NGD94-1 modulates the cognitive functions of the frontostriatal system and regulates dopaminergic transmission in Phencyclidine (PCP)-induced monkeys. NGD94-1 can be used for neurological disease research [1][2].
GS-8873 TFA is the TFA salt form of GS-8873 (HY-145713). GS-8873 TFA is an orally active inhibitor for the production of hepatitis B virus (HBV) surface antigen (HBsAg) with an EC50 of 4 nM. GS-8873 TFA exhibits good pharmacokinetic characters in rats and metabolic stability in human hepatocytes. GS-8873 TFA causes neurofunctional deficits in rats and cynomolgus monkeys .
U-90042 is a gamma-aminobutyric acidA receptor agonist of α1, α3 and α6 subtypes with Ki values of 7.8 nM, 9.5 nM and 11.0 nM, respectively. U-90042 suppresses locomotor activity and impairs rotarod performance in mice. U-90042 produces sedation and ataxia and prolongs sleeping time in mice, rats and monkeys. U-90042 can be used as a sedative and hypnotic agent .
PD-134672 (CI-992) is a renin inhibitor containing a 2-amino-4-thiazolyl substituent. PD-134672 potently inhibits monkey renin in vitro and only weakly inhibits the related aspartic protease bovine feline hepsin D. The compound exhibits oral hypotensive activity in hyperreninemic normotensive monkeys. Based on its superior efficacy and long-lasting effects in vitro and in the normotensive macaque model, PD-134672 was selected for further evaluation in renal hypertensive monkeys.
RL-37 is an alpha-helical antimicrobial peptide. RL-37 can be isolated for rhesus monkey bone marrow. RL-37 rapidly permeabilizes the membranes of Escherichia coli ML-35p and lysed liposomes. RL-37 has effective antibacterial activity against staphylococci, such as wild-type and Methicillin (HY-121544)-resistant S. aureus strains and S. epidermidis ATCC 49741. RL-37 can be used for human skin infections research .
PGF2α 1,15-lactone (Prostaglandin F2α 1,15-lactone) is a lipid-soluble internal ester of PGF2α. PGF2α 1,15-lactone decreases menstrual cycle lengths in non-pregnant rhesus monkeys. PGF2α 1,15-lactone terminates early pregnancy in the monkey .
Mirincamycin (hydrochloride) (U-24729 A), a compound used to inhibit malaria, has a protective effect against the early liver stages of Plasmodium but fails to kill dormant liver stages of Plasmodium in a rhesus monkey model.
SMP-88480 is an Antibody-Drug Conjugates (ADCs). SMP-88480 is stable in mouse, monkey and human plasma and has in vivo tumor inhibitory effects on ovarian cancer, gastric cancer, and breast cancer .
SQ 31844 is a novel renin inhibitor belonging to the imidazolidinol class. This compound, which contains an imidazole ring in its active site binding group, has potent in vitro inhibition of primate renin, but not rat, pig, or dog renin. In conscious, sodium-deprived cynomolgus monkeys, both compounds produced dose-related inhibition of plasma renin activity (PRA) over a dose range of 0.001 to 1.0 μmol/kg, administered intravenously, with complete inhibition observed at the highest dose. However, a reduction in blood pressure was only observed when 10 μmol/kg was administered intravenously or by infusion. In sodium-replete monkeys, SQ 30774 inhibited the increase in arterial blood pressure and PRA following administration of exogenous monkey renin. When the compounds were administered orally at 50 μmol/kg, only SQ 31844 significantly inhibited PRA (80%). In summary, the imidazolidinol renin inhibitors have potent inhibitory effects on renin in vitro and inhibit PRA and reduce arterial blood pressure in vivo.
Cynomolgus Monkey haptoglobin is a hemoglobin-binding protein derived from cynomolgus monkeys. Cynomolgus Monkey haptoglobin is generally assumed to be analogous to human serum haptoglobin (Hp) .
Cynomolgus Monkey transferrin is a cynomolgus monkey-derived protein. Transferrin is the transport of iron in the bloodstream. Transferrin can also act as a growth factor .
Anti-Human/Monkey NKG2D Antibody (ON72) is an antibody targeting human/monkeyNKG2D. The isotype control for Anti-Human/Monkey NKG2D Antibody (ON72) can be referenced as Mouse IgG1 kappa, Isotype Control (HY-P99977).
Anti-Human/Monkey NKG2D Antibody (16F16) is an antibody targeting human/monkeyNKG2D. The isotype control for Anti-Human/Monkey NKG2D Antibody (16F16) can be referenced as Human IgG4 kappa, Isotype Control (HY-P99003).
Type II Collagen, T Cell Grade, from Monkey is a T-cell dependent antigen with unique immunological features. Type II Collagen, T Cell Chick, from Monkey can be used as a stimulating antigen for T-cells in in vitro culture systems .
Anti-Human/Monkey CXCR4 Antibody (12G5) reacts with human and monkey CXCR4. Anti-Human/Monkey CXCR4 Antibody (12G5) blocks the cognate ligand, CXCL12/SDF-1, and gp120/160 from binding to CXCR4. Recommend Isotype Controls: Mouse IgG2a kappa, Isotype Control (HY-P99978) .
Anti-Human/Monkey CD16a Antibody (3G8) is a monoclonal antibody targeting CD16a. Anti-Human/Monkey CD16a Antibody (3G8) blocks FcγRIII/CD16a, upregulates the metabolic activity of CD16+ cells, downregulates CD87, a poor prognostic marker, and inhibits the engraftment and growth of leukemia cells in acute myeloid leukemia, and rapidly increases platelet counts in immune thrombocytopenia. Anti-Human/Monkey CD16a Antibody (3G8) is applicable to research related to tumor immunology .
Anti-Human/Mouse/Monkey CXCR3 Antibody (9C5) is an antibody targeting CXCR3, which specifically binds to an epitope within amino acid residues 23 to 44 of human CXCR3 .
AZD3676 is an orally active and blood-brain barrier-permeable ligand for 5-HT1A and 5-HT1B receptors, with nanomolar binding affinity for human and monkey receptors (human 5-HT1A: 0.16 nM, monkey 5-HT1A: 0.13 nM, human 5-HT1B: 2.3 nM, monkey 5-HT1B: 2.4 nM). AZD3676 is applicable to research related to cognitive impairment in Alzheimer's disease .
TASP0434299 (Compound 10) is a radiolabeled ligand for the vasopressin V1b receptor. TASP0434299 exhibits high binding affinity for human and murine V1B receptors, with IC50 values of 0.526 nM and 0.641 nM, respectively, and shows potent antagonistic activity against the human V1B receptor with an IC50 of 0.639 nM. TASP0434299 is a substrate for human and rhesus monkeyP-glycoprotein, resulting in low brain uptake in rhesus monkeys. TASP0434299 binds to V1B receptors in rat and monkey pituitary tissues in a saturable and specific manner both in vitro and in vivo. When radiolabeled with tritium or 11C, TASP0434299 serves as a prototype V1B receptor radiotracer to visualize V1B receptor in the pituitary gland of anesthetized monkeys via positron emission tomography .
TPP-9476 is an anti-human IL3RA (CD123) monoclonal antibody with human IL3RAKd of 11 nM and cynomolgus monkeyIL3RAKd of 16 nM. TPP-9476 binds specifically to human and cynomolgus monkeyIL3RA, undergoes target-dependent internalization into lysosomes of IL3RA-positive cells.TPP-9476 exerts antiproliferative effects in IL3RA-expressing acute myeloid leukemia and classical Hodgkin lymphoma cells, reduces tumor burden, improves survival, and induces complete tumor remission in relevant xenograft mouse models .
AMY109 is an anti-human interleukin-8 (IL-8) monoclonal antibody, with IC50 values of 0.14 μg/mL and 0.37 μg/mL against human IL-8, a Ka of 36.8 pM for human IL-8, and a Ka of 380 pM for cynomolgus monkey IL-8.\nAMY109 binds to human and cynomolgus monkey IL-8 in a pH-dependent manner, inhibits IL-8-mediated activation of CXCR1 and CXCR2, and blocks the downstream biological activities of IL-8. AMY109 inhibits neutrophil recruitment to endometriotic lesions and suppresses monocyte chemoattractant protein-1 production by neutrophils. AMY109 is applicable to research related to endometriosis .
LY2775240 is an orally active phosphodiesterase 4 (PDE4) inhibitor with potent inhibitory activity against PDE4A (IC50 = 0.09 nM), PDE4B (IC50 = 0.09 nM) and PDE4D (IC50 = 0.14 nM), and exhibits an IC50 of 2.4 nM against PDE4C. LY2775240 is a highly selective agent that reduces TNFα production upon immune activation. LY2775240 decreases TNFα production in rodent and rhesus monkey models. LY2775240 can be used in the research of psoriasis .
GSK2394002 is an antibody inhibitor targeting ADAMTS-4 and ADAMTS-5, with cartilage-penetrating ability following systemic administration. GSK2394002 inhibits the release of aggrecan-derived neoepitopes and reduces cartilage degradation, exhibiting the potential to relieve pain, alleviate hyperalgesia and inhibit the progression of joint damage. GSK2394002 also induces potentially irreversible cardiovascular effects such as increased mean arterial pressure and myocardial ischemia in cynomolgus monkeys .
HZD37-5 is a humanized monoclonal antibody specifically recognizing N78 loci of IL-17A. HZD37-5 binds to human and rhesus monkeys, blocks IL-17 induced signal transduction and the release of IL-6, IL-8, CXCL-1 and GM-GSF.HZD37-5 significantly inhibited human IL-17A induced-keratinocyte chemoattractant secretion. HZD37-5 can be used for the research of autoimmune diseases including psoriasis and psoriatic arthritis .
MK-5661 is an orally potent NaV1.8 voltage-gated sodium channel inhibitor with an EC50 of 4.3 nM. MK-5661 selectively inhibits peripheral nociceptive signaling mediators. MK-5661 reduces capsaicin-induced spontaneous nociceptive behaviors in humanized rats and attenuates capsaicin-induced skin flushing responses in rhesus monkeys. MK-5661 is applicable for pain-related research .
A-62198 is a potent and selective renin inhibitor with antihypertensive activity. A-62198 reduces mean arterial pressure (MAP) in anesthetized, salt-deprived monkeys in a dose-dependent manner. A-62198 induced MAP reduction in normal monkeys that reached statistical significance at the highest dose and significantly inhibited plasma renin activity (PRA) at all doses .
IBI352g4a is a humanized IgG1 monoclonal antibody targeting PVRIG (Kd = 0.53 nM) and acts as a PVRIG/PVRL2 inhibitor. The anti-tumor effect of IBI352g4a depends on the binding of its Fc region to FcγR. IBI352g4a binds to the extracellular domains of human and cynomolgus monkey PVRIG, and blocks the PVRIG-PVRL2 interaction. IBI352g4a induces NK cell activation, promotes their degranulation and tumor killing. IBI352g4a can be used in the research of gastric cancer .
Prodilidine (CI-427) is an orally active, pyrrolidine-derived non-narcotic pain inhibitor. Prodilidine exerts analgesic activity against various nociceptive stimuli, and shows no antipyretic, anti-inflammatory or respiratory depressive effects. Prodilidine fails to inhibit withdrawal symptoms of addictive agents in monkeys, but exhibits excitatory effects and enhances the crossed extensor reflex at toxic doses. Prodilidine is well absorbed from the gastrointestinal tract and metabolized via hepatic microsomal N-demethylation, displaying isomer-specific activity, toxicity and metabolic characteristics. Prodilidine can be used in research related to chronic pain (e.g., cancer-, musculoskeletal/arthritis-derived), traumatic pain and arthritic pain .
5-Monobutyl methotrexate (NSC 305986; γ-MBMTX) is a dihydrofolate reductase (DHFR) inhibitor and esterase substrate. 5-Monobutyl methotrexate is hydrolyzed by esterases to produce methotrexate. In rhesus monkeys, 5-Monobutyl methotrexate clears more slowly from cerebrospinal fluid than from serum, and its serum protein binding rate exceeds 99%. At the same dose rate, 5-Monobutyl methotrexate achieves cerebrospinal fluid concentrations comparable to those of Methotrexate (HY-14519), and exhibits activity against Methotrexate-resistant cells (with transport defects) that is comparable to that against sensitive parental cells. 5-Monobutyl methotrexate can be used in studies related to Methotrexate-resistant tumors .
RC98 is a monoclonal antibody targeting programmed cell death ligand 1 (PD-L1) and acts as a selective PD-L1 inhibitor. RC98 binds specifically to human and cynomolgus monkey PD-L1. RC98 blocks the interaction between PD-L1 and its receptor PD-1 to reverse T-cell inactivation mediated by PD-1/PD-L1 signaling. RC98 enhances the cytotoxic T-lymphocyte-mediated anti-tumor immune response against PD-L1-expressing tumor cells. RC98 can be used for the research of tumor immunity and solid tumors .
PF-03475952 is a fully human IgG2 monoclonal antibody targeting CD44. PF-03475952 binds an epitope in CD44’s constant exons, blocks CD44-hyaluronic acid interaction, reduces cell surface CD44, and does not cross-react with rodent CD44 or LYVE-1. PF-03475952 induces cancer cell apoptosis, inhibits LPS (HY-D1056)-induced leukocyte cytokine release and cancer metastasis, and reduces CD44 expression on circulating CD3+ lymphocytes in cynomolgus monkeys. PF-03475952 can be used for the research of rheumatoid arthritis and hepatocellular carcinoma .
SK48-E26 is a human interleukin-1β (IL-1β) inhibitor, with a IC50 of 400 pM against human IL-1β, a IC50 of 185 pM against cynomolgus monkey IL-1β, and a Ka value ranging from 0.048 nM to 3 nM for human IL-1β. SK48-E26 binds to the conformational epitope of human IL-1β spanning amino acid residues 95-101, and blocks the biological activity of IL-1β. SK48-E26 can be used in research related to IL-1β-mediated inflammatory diseases and osteoarthritis .
TPPU (Standard) is the analytical standard of TPPU (HY-101294). This product is intended for research and analytical applications. TPPU is a soluble epoxide hydrolase (sEH) inhibitor with IC50 values of 37 and 3.7 nM for monkey and human sEH, respectively.
FCE 28654 is an inhibitor of acylCoA: cholesterol acyltransferase (ACAT), weakly inhibiting ACAT in microsomes from rabbit aorta and intestine, and monkey liver, with IC50s of 2.55, 1.08 and 5.69 μM, respcetively.
SDZ-CPI-975 is a novel, reversible, and selective CPT I inhibitor. SDZ-CPI-975 effectively inhibits fatty acid oxidation and lowers blood glucose levels .
7-Methylxanthine is an orally active methyl derivative of xanthine and a non-selective adenosine receptor antagonist. 7-Methylxanthine is also one of the purine components of human urinary calculi. 7-Methylxanthine has anti-myopia activity .
BMS-181101 (hydrochloride) is an orally active antidepressant. BMS-181101 (hydrochloride) can interact with a variety of central presynaptic and postsynaptic 5-HT receptors. BMS-181101 (hydrochloride) can be used in the research of diseases such as depression .
Nesfrotamig (YH32367; ABL105) is a bispecific activator targeting HER2 and 4-1BB. The Kd values of Nesfrotamig for human HER2 and human 4-1BB are 0.48 nM and 3.36 nM, respectively. By blocking tumor cell growth signals, activating HER2-dependent local 4-1BB in tumors to maintain T cell survival, and inducing NK cell-mediated antibody-dependent cellular cytotoxicity, Nesfrotamig enhances the cytotoxicity and tumor infiltration ability of immune cells. Nesfrotamig promotes the generation of tumor-specific memory T cells, drives T cell-mediated tumor lysis, exhibits significant anti-tumor efficacy against both HER2-positive and HER2-low-expressing tumors, and shows synergistic activity when combined with anti-PD-1 antibodies. In cynomolgus monkey studies, Nesfrotamig demonstrates good safety and is suitable for research related to HER2-positive and HER2-low-expressing tumors .
WR-27653 (RC-12) is a derivative of Catechol with good activity against hypnozoites in the gold-standard Plasmodium cynomolgi-rhesus monkey (Macaca mulatta) model. WR-27653 has antimalarial activity .
CDP-840 (GR259653X) is a potent, selective and orally active phosphodiesterase IV (PDE IV) inhibitor. CDP-840 inhibits antigen-induced early and late phase bronchoconstriction in conscious squirrel monkeys .
MB-07344 sodium is a potent thyroid hormone receptor (TR)-β agonist with a Ki of 2.17 nM. MB-07344 sodium has additive cholesterol lowering activity in combination with Atorvastatin (HY-B0589) in rabbits, dogs and monkeys .
VU0467154 is a positive allosteric modulator of the M4 muscarinic acetylcholine receptor (mAChR), potentiating the response to ACh with pEC50s of 7.75, 6.2 and 6 for rat, human and cynomolgus monkey M4 receptor, respectively.
Fluoroclebopride binds reversibly to dopamine receptors. 18F labeled fluoroclebopride has been used as a probe for studying D2/D3 receptor availability via PET in various monkey models .
MB-07344 is a potent thyroid hormone receptor (TR)-β agonist with a Ki of 2.17 nM. MB-07344 has additive cholesterol lowering activity in combination with Atorvastatin (HY-B0589) in rabbits, dogs and monkeys .
MT204 is a humanized IgG1 antibody inhibitor targeting IL-2 of human and rhesus monkey origin. MT204 prevents soluble IL-2 from binding to intermediate-affinity IL-2 receptors and blocks CD25-bound IL-2 on high-affinity IL-2 receptors. MT204 has potently anti-proliferative activity with NKL cells and primary NK cells. MT204 has good tolerability and potent immunosuppressive activity in allogeneic skin graft model of rhesus monkey, promising for immunosuppressive and anti-proliferative therapy .
Anrukinzumab (IMA-638) is a humanized anti-IL-13 monoclonal antibody. Anrukinzumab effectively reduces lung inflammation in a cynomolgus monkey model. Anrukinzumab can be used in studies of ulcerative colitis (UC) as well as asthma .
Artemotil (β-Arteether) has antimalarial activity for the treatment of chloroquine-resistant Plasmodium falciparum malaria with an IC50 of 1.61 nM. Artemotil also has central nervous system (CNS) neurotoxicity and anorectic toxicity in rats, dogs and monkeys .
Auranofin (SKF-39162) is a thioredoxin reductase (TrxR) inhibitor with an IC50 of 0.2 μM. Auranofin exhibits antiviral activity against SARS-CoV21, with a CC50 of 4.2 μM for monkey kidney Vero E6 cells.
Navarixin (SCH 527123) is a potent, allosteric and orally active antagonist of both CXCR1 and CXCR2, with Kd values of 41 nM for cynomolgus CXCR1 and 0.20 nM, 0.20 nM, 0.08 nM for mouse, rat and cynomolgus monkey CXCR2, respectivelly .
(R)-RS 56812 hydrochloride is a 5-HT3 receptor antagonist that enhances performance in monkeys on a delayed matching task. The (R) isomer produces more systematic improvements than the (S) isomer and has potential inhibitory effects in diseases involving cognitive decline.
(R)-RS 56812 is a 5-HT3 receptor antagonist that enhances performance in monkeys on a delayed matching task. The (R) isomer produces more systematic improvements than the (S) isomer and has potential inhibitory effects in diseases involving cognitive decline.
Desmethyl bosentan is an active metabolite of the endothelin receptor antagonist bosentan (HY-A0013).1 Desmethyl bosentan (25 μM) activates the pregnane X receptor (PXR) in CV-1 monkey kidney cells expressing the human receptor in a reporter assay.
5-MCA-NAT is a melatonin agonist that may target the melatoninMT3 receptor. 5-MCA-NAT can contract the colonic band in a concentration-dependent manner and reduce intraocular pressure (IOP) in glaucomatous monkey eyes, inhibiting the increase in IOP .
H-0104 dihydrochloride is a ROCK inhibitor with significant intraocular pressure (IOP)-lowering activity. H-0104 dihydrochloride effectively reduces IOP when administered to monkey eyes. There may not be a direct relationship between the Iop-lowering effect of H-0104 dihydrochloride and ROCK inhibition .
Visugromab (CTL-002) is a GDF-15 neutralizing IgG4 mAb. Visugromab has synergistic anticancer activity with the anti-PD1 antibody Nivolumab (HY-P9903) and can effectively act on PD-1/PD-L1 relapsed/refractory metastatic solid tumors. Recommend Isotype Controls: Human IgG4 (S228P) kappa, Isotype Control (HY-P99003) .
GLP-1R agonist 28 (Compound 19) is an orally active GLP-1R agonist. GLP-1R agonist 28 can increase insulin secretion and can be used in the research of GLP-1R-related diseases .
Visugromab (CTL-002) (Powder) is a GDF-15 neutralizing IgG4 mAb. Visugromab (Powder) has synergistic anticancer activity with the anti-PD1 antibody Nivolumab (HY-P9903) and can effectively act on PD-1/PD-L1 relapsed/refractory metastatic solid tumors. Recommend Isotype Controls: Human IgG4 (S228P) kappa, Isotype Control (HY-P99003) .
LSN3353871 is a potent inhibitor of lipoprotein(a) (Lp(a)) that can binds to Kringle IV (KIV) 8, KIV7-8 and KIV5-8, with Kd of 756 nM, 605 nM and 423 nM, respectively. LSN3353871 disrupts the formation of Lp(a) with the IC50 of 1.69 μM. LSN3353871 has oral bioactivity .
Zampilimab (UCB-7858) is a monoclonal antibody against transglutaminase 2 (TG2). Zampilimab inhibits TG2 crosslinking transamidation activity with an IC50 of 0.25 nM and a Kd of <50 pM. Zampilimab improves renal fibrosis .
BMS-986120 is a first-in-class oral and reversible protease-activated receptor 4 (PAR4) antagonist, with IC50s of 9.5 nM and 2.1 nM in human and monkey blood, respectively. BMS-986120 has potent and selective antiplatelet effects .
PAM 1392 is active orally against Plasmodium berghei in mice, P. cynofologi and P. knowlesi in monkeys and Trypanosoma cruzi in tissue cultures of mice, and hemolytic streptococci in vitro. PAM 1392 has antimalarial and antitrypanosomal activities, which is proming for rasearch of drug-resistant malaria .
Rev 6207 (free base) is a potent non-thiol angiotensin I converting enzyme inhibitor. Rev 6207 (free base) has comparable antihypertensive activity to Enalapril (HY-B0331) in awake monkeys with high renin activity and can be used in the study of hypertensive diseases .
Isoxepac (Standard) is the analytical standard of Isoxepac. This product is intended for research and analytical applications. Isoxepac (HP 549) is a nonsteroidal anti-inflammatory agent (NSAID) with anti-inflammatory, analgesic and antipyretic activity. Isoxepac has been studied in rat, rabbit, dog, rhesus monkey, etc .
CL-283796 is a potent and orally active acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor. CL-283796 reduces low-density lipoprotein (LDL) cholesterol without affecting cholesterol absorption in African green monkeys. CL-283796 can be used for hypercholesterolemia research .
MK-0668 is an amino acid-based, potent antagonist of unactivated VLA-4, with an IC50) of 0.13 nM in human whole blood. And MK-0668 exhibits IC50s of 0.19 nM in dogs, 0.21 nM in rhesus monkeys, and 0.4 nM in rats .
MK-0668 mesylate is an amino acid-based, potent antagonist of unactivated VLA-4, with an IC50) of 0.13 nM in human whole blood. And MK-0668 mesylate exhibits IC50s of 0.19 nM in dogs, 0.21 nM in rhesus monkeys, and 0.4 nM in rats .
GSK2982772 (Standard) is the analytical standard of GSK2982772 (HY-101760). This product is intended for research and analytical applications. GSK2982772 is a potent, orally active and ATP competitive RIP1 kinase inhibitor with IC50 values of 16 nM and 20 nM for human and monkey RIP1, respectively .
Cevoglitazar (LBM-642) is an orally active and highly potent PPARα and PPARγ dual agonist. Cevoglitazar can reduce food intake, body weight, and fasting plasma insulin in obese mice and cynomolgus monkeys. Cevoglitazar has the potential for diabetes and obesity-related disorders research .
Tetramethylpyrazine nitrone is a nitrone derivative of tetramethylpyrazine. Tetramethylpyrazine nitrone is an active ingredient from Ligusticum wallichii Franchat. Tetramethylpyrazine nitrone is a potent scavenger of free radicals with neuroprotective activitys in both rat and monkey models of ischemis stroke. Tetramethylpyrazine nitrone can suppress over-expression of neuroinflammatory marker vimentin .
BAY-298 is an orally active and selective luteinizing hormone receptor (LH-R) antagonist with IC50s of 96 nM, 23 nM and 78 nM for hLH (human LH) and rLH (rat LH) and cLH (cynomolgus monkey LH), respectively. BAY-298 can reduce sex hormone levels .
Mefenidil (MCN 2378) is a selective cerebral vasodilator that is not affected by beta-adrenergic blockade. Mefenidil can be used in the study of cardiovascular disease. In monkey models, mefenidil preferentially increases cerebral blood flow over systemic (femoral) blood flow. Mefenidil is also able to reduce systemic arterial pressure in anesthetized dogs.
GDC-6599 is an orally active TRPA1 inhibitor, with IC50 values of 5.3 nM in humans, 6.6 nM in rats, 9.3 nM in dogs, 7.2 nM in monkeys, and 15 nM in guinea pigs. GDC-6599 can be used in the research of neuropathic pain and respiratory diseases such as asthma and chronic cough .
17-Phenyl trinor 8-iso prostaglandin E2 is a prostaglandin analog that reduces intraocular pressure (IOP) in both normal and glaucomatous monkey eyes. 17-Phenyl trinor 8-iso prostaglandin E2 lowers IOP primarily by increasing trabecular outflow facility .
Apilimod (STA 5326) is a potent IL-12/IL-23 inhibitor, and strongly inhibits IL-12 with IC50s of 1 nM and 2 nM, in IFN-γ/SAC-stimulated human PBMCs and SAC-treated monkey PBMCs, respectively . Apilimod is a potent and highly selective PIKfyve inhibitor.
Apilimod (STA 5326) mesylate is a potent IL-12/IL-23 inhibitor, and strongly inhibits IL-12 with IC50s of 1 nM and 2 nM, in IFN-γ/SAC-stimulated human PBMCs and SAC-treated monkey PBMCs, respectively . Apilimod is a potent and highly selective PIKfyve inhibitor.
Ubrogepant (MK-1602) is an orally active and selective antagonist of calcitonin gene-related peptide receptor (CGRP). Ubrogepant has high affinity for CGRP receptors in human and rhesus monkeys, and can effectively block the cAMP response stimulated by α-CGRP. Ubrogepant can be used in the study of acute migraine .
BAM-1110 is a dopamine receptor agonist. BAM-1110 exhibits dose-dependent antiparkinsonian activity in MPTP (HY-W114750)-treated monkey models of Parkinson's disease. BAM-1110 has minimal side effects and can be used for the research of Parkinson's disease and other neurological disorders .
Auranofin (Standard) is the analytical standard of Auranofin. This product is intended for research and analytical applications. Auranofin (SKF-39162) is a thioredoxin reductase (TrxR) inhibitor with an IC50 of 0.2 μM. Auranofin exhibits antiviral activity against SARS-CoV21, with a CC50 of 4.2 μM for monkey kidney Vero E6 cells.
L-751788 is a selective inhibitor of type I of 5α-reductase. L-751788 does not have a significant impact on the differentiation of the external genitalia in animals. When administered orally to pregnant rhesus monkeys, L-751788 (2, 10 mg/kg) did not cause abnormalities in fetal external genitalia .
Hydroxyprogesterone caproate (Standard) is the analytical standard of Hydroxyprogesterone caproate. This product is intended for research and analytical applications. Hydroxyprogesterone caproate (17α-Hydroxyprogesterone hexanoate; 17α-Hydroxyprogesterone caproate) is a progesterone receptor (progesterone receptor) ligand and steroid hormone transcription inhibitor. Hydroxyprogesterone caproate downregulates estrogen receptors in target tissues and activates their metabolic pathways, and exhibits equivalent affinity for progesterone receptor A and progesterone receptor B. Hydroxyprogesterone caproate shows no consistent teratogenicity or developmental toxicity in rat, mouse and monkey models, but induces resorption or abortion in rhesus monkeys at human-equivalent doses. Hydroxyprogesterone caproate promotes the production of TNF-α in lipopolysaccharide-stimulated whole blood from non-pregnant women. Hydroxyprogesterone caproate can be used in scientific research related to preterm birth .
Orforglipron (LY3502970) (Compound 67) is an orally active agonist for Glucagon-like peptide-1 receptor (GLP-1R), which exhibits potency in ameliorates the type 2 diabete .
MK-8768 is a highly potent, orally bioavailable and selective class of mGluR2negative allosteric modulator (IC50 of 9 .6nM) with excellent brain permeability.
Orforglipron hemicalcium hydrate (LY3502970 hemicalcium hydrate; GLP-1 receptor agonist 1 hemicalcium hydrate) is the calcium salt hydrate form of Orforglipron (HY-112185). Orforglipron is an orally active agonist for Glucagon-like peptide-1 receptor (GLP-1R), which exhibits potency in ameliorating the type 2 diabete .
uPSEM792 is a pharmacologically selective effector molecules (PSEM) agonist for PSAM 4-GlyR, with an affinity of Ki of 0.7 nM. uPSEM792 is a substrate for efflux transporters in brains of wild type and dual P-gp and BCRP knockout mice. uPSEM7952 is a possible lead for developing the PET radioligand for PSAM 4-GlyR .
9-Keto Travoprost is a derivative of Fluprostenol (HY-108560). 9-Keto Travoprost is an EP receptor agonist. 9-Keto Travoprost can be used in endocrine-related research .
SCH-602539 is a selective PAR-1 antagonist. SCH-602539 inhibits platelet aggregation in response to PAR-1-selective high-affinity thrombin receptor agonist peptide. SCH-602539 exhibits synergistic antithrombotic effects when used in combination with Cangrelor (HY-19638) .
BMS-351 (compound 18) is a potent, oral active, nonsteroidal CYP17A1 lyase inhibitor with the IC50 values of 19 nM and 4 nM aganist human CYP17A1 and cynomolgus monkeys CYP17A1,respectively. BMS-351 can be used for the study of castration-resistant prostate cancer .
Arevirumab (Arevirumab-3) is a pan-lineage neutralizing human monoclonal antibody cocktail (8.9F, 12.1F, 37.D). Arevirumab protects cynomolgus monkeys from severe Lassa fever caused by lineage II and III LASV isolates. Arevirumab is applicable to research related to Lassa fever .
CJB-090 dihydrochloride is a partial agonist with activity at dopamine D3 receptors. CJB-090 exhibits partial agonist characteristics in vitro. CJB-090 elicits yawning responses only in monkeys with an extensive history of cocaine use. CJB-090 reduces the reinstatement effects of cocaine in reinstatement behaviors induced by cocaine .
NW-1172 (free base) (compound 22b) is a 5-HT3 receptor antagonist with performance-enhancing activity in a delayed matching task in monkeys, with the (R) isomer producing more systematic improvements than the (S) isomer, a difference paralleled by the higher affinity of the (R) enantiomer for the 5-HT3 receptor.
Lanraplenib (GS-9876) is a highly selective and orally active SYK inhibitor (IC50=9.5 nM) in development for the treatment of inflammatory diseases. Lanraplenib (GS-9876) inhibits SYK activity in platelets via the glycoprotein VI (GPVI) receptor without prolonging bleeding time (BT) in monkeys or humans .
RO4583298 is a potent, orally active dual antagonist of NK1 (human and gerbil)/NK3 (human, cynomolgus monkey, gerbil and guinea-pig). RO4583298 inhibits senktide-induced potentiation of spontaneous activity of dopaminergic neurons. RO4583298 can block gerbil foot tapping response and inhibits mouse tail whips .
H-0106 dihydrochloride is a ROCK inhibitor with potent intraocular pressure (IOP)-lowering activity. H-0106 dihydrochloride can effectively inhibit ROCK enzyme. H-0106 dihydrochloride demonstrated significant IOP-lowering effects in monkey eyes. Studies with H-0106 dihydrochloride suggest that there may not be a direct relationship between ROCK inhibition and IOP reduction .
(R)-BMS-816336 (Compound 6n-1) is a potent and orally active inhibitor of human, mouse and cynomolgus monkey 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) enzyme with IC50s of 14.5 nM, 50.3 nM and 16 nM, respectively .
Remikiren (Ro 42-5892) is an orally active and highly specific renin inhibitor. Remikiren specifically inhibits human reninand human plasma renin with IC50 values of 0.7 and 0.8 nM, respectively. Remikiren also reduces mean arterial blood pressure in sodium-depleted marmosets and squirrel monkeys. Remikiren can be used in study of hypertension .
Xaluritamig (AMG-509) is a bispecific T cell engager and cytolytic agent with a Kd of 27.6 nM for human CD3ε. Xaluritamig binds to CD3ε via an anti-CD3 single-chain variable fragment (scFv) domain, and to STEAP1 via a bispecific anti-STEAP1 antigen-binding fragment (Fab) domain, thereby recruiting and activating T cells and forming a bridge between T cells and STEAP1-expressing cancer cells. Xaluritamig induces T cell-mediated redirected cytotoxicity, tumor cell lysis, cytokine release, CD8 + T cell activation and expansion, as well as tumor stasis or regression. Xaluritamig contains an Fc domain with no effector function, which prolongs serum half-life, exhibits only minimal activity against cells with low STEAP1 expression and normal cells, and shows extremely low target-related off-tumor toxicity in cynomolgus monkeys. Xaluritamig is used in STEAP1×CD3 XmAb 2+1 immunotherapy and in research on metastatic castration-resistant prostate cancer and Ewing sarcoma .
Forodesine (BCX-1777) is a highly potent and orally active purine nucleoside phosphorylase (PNP) inhibitor with IC50 values ranging from 0.48 to 1.57 nM for human, mouse, rat, monkey and dog PNP. Forodesine is a potent human lymphocyte proliferation inhibitor. Forodesine could induce apoptosis in leukemic cells by increasing the dGTP levels .
Forodesine hydrochloride (BCX-1777 hydrochloride) is a highly potent and orally active purine nucleoside phosphorylase (PNP) inhibitor with IC50 values ranging from 0.48 to 1.57 nM for human, mouse, rat, monkey and dog PNP. Forodesine hydrochloride is a potent human lymphocyte proliferation inhibitor. Forodesine hydrochloride could induce apoptosis in leukemic cells by increasing the dGTP levels .
FZ-AD005 is a DLL3-targeting antibody-drug conjugate (ADC) with high selectivity, composed of the anti-DLL3 antibody FZ-A038 (HY-P990896), a dipeptide linker (Val-Ala), and DXd (HY-13631D). The Kd value of FZ-AD005 for human DLL3 ranges from 13.29 to 58.3 pmol/L. After binding to DLL3 on the cell surface, FZ-AD005 mediates endocytosis, and the payload DXd is released via cleavage by lysosomal cathepsins. DXd inhibits topoisomerase TopI to induce double-strand DNA breaks, cell cycle arrest and apoptosis, and FZ-AD005 exhibits bystander killing activity against adjacent DLL3-negative cells. FZ-AD005 shows stable circulation in vivo, has good tolerance and acceptable pharmacokinetic profiles in rats and cynomolgus monkeys, and effectively inhibits the growth of DLL3-expressing tumor cells. FZ-AD005 serves as a promising candidate molecule for research on small cell lung cancer and human neuroendocrine prostate cancer .
Hydroxyprogesterone caproate-d8 (17α-Hydroxyprogesterone hexanoate-d8) is the deuterium labeled Hydroxyprogesterone caproate (HY-B0742). Hydroxyprogesterone caproate (17α-Hydroxyprogesterone hexanoate; 17α-Hydroxyprogesterone caproate) is a progesterone receptor (progesterone receptor) ligand and steroid hormone transcription inhibitor. Hydroxyprogesterone caproate downregulates estrogen receptors in target tissues and activates their metabolic pathways, and exhibits equivalent affinity for progesterone receptor A and progesterone receptor B. Hydroxyprogesterone caproate shows no consistent teratogenicity or developmental toxicity in rat, mouse and monkey models, but induces resorption or abortion in rhesus monkeys at human-equivalent doses. Hydroxyprogesterone caproate promotes the production of TNF-α in lipopolysaccharide-stimulated whole blood from non-pregnant women. Hydroxyprogesterone caproate can be used in scientific research related to preterm birth .
AGN 191976 is a potent and selective thromboxane A2-sensitive (TP) receptor agonist with EC50 values of 0.23 nM and 24 nM in rat aorta and human platelets, respectively. AGN 191976 has potent IOP-lowering effects in dogs and monkeys. AGN 191976 can be used to study vascular biology and the role of thromboxane A2 in vascular function .
Guanfu base A hydrochloride is an antiarrhythmic alkaloid with the ability to inhibit CYP2D6 enzyme activity. Guanfu base A hydrochloride can be used to inhibit arrhythmia-related diseases. Guanfu base A hydrochloride exhibits inhibitory effects on CYP2D6 in different species of organisms, including humans, monkeys, and dogs. The biological activity of Guanfu base A hydrochloride makes it have potential clinical application value .
IMA-1 is an inhibitor that inhibits the interaction between arachidonic acid 12-lipoxygenase (ALOX12) and acetyl-CoA carboxylase 1 (ACC1). IMA-1 significantly blocks the progression of diet-induced non-alcoholic steatohepatitis (NASH) in male mice and crab-eating monkeys, and does not cause hyperlipidemia. IMA-1 can be used for the study of NASH .
Navarixin (Standard) is the analytical standard of Navarixin (HY-10198). This product is intended for research and analytical applications. Navarixin (SCH 527123) is a potent, allosteric and orally active antagonist of both CXCR1 and CXCR2, with Kd values of 41 nM for cynomolgus CXCR1 and 0.20 nM, 0.20 nM, 0.08 nM for mouse, rat and cynomolgus monkey CXCR2, respectivelly .
Ponsegromab is a Growth differentiation factor 15 (GDF15) inhibitor with human, cynomolgus monkey, and mouse target IC50 values of 0.123 nM, 0.053 nM, and 0.102 nM, respectively . Ponsegromab acts as a chemosensitizer, increases intracellular reactive oxygen species, reduces glutathione levels . Ponsegromab can be used for the research of oxaliplatin-resistant colorectal cancer .
Lanraplenib succinate (GS-9876 succinate) is a highly selective and orally active SYK inhibitor (IC50=9.5 nM) in development for the treatment of inflammatory diseases. Lanraplenib succinate (GS-9876 succinate) inhibits SYK activity in platelets via the glycoprotein VI (GPVI) receptor without prolonging bleeding time (BT) in monkeys or humans .
(rac)-AL-37350A ((rac)-4,5-DHP-AMT) is a 5-HT2 receptor agonist with intraocular pressure-lowering activity. (rac)-AL-37350A has high affinity and selectivity for the 5-HT2 receptor and effectively reduces intraocular pressure in conscious hypertensive cynomolgus monkeys.
SB-657510 is a selective urotensin II (UII) receptor (UT) antagonist. The Ki values are 61, 17, 30, 65 and 56 nM for human, monkey, cat, rat and mouse receptors, respectively. SB-657510 exerts anti-inflammatory effects by inhibiting UII-induced upregulation of inflammatory mediators such as adhesion molecules, cytokines, and tissue factor in human vascular endothelial cells .
Lanraplenib monosuccinate (GS-9876 monosuccinate) is a highly selective and orally active SYK inhibitor (IC50=9.5 nM) in development for the treatment of inflammatory diseases. Lanraplenib monosuccinate (GS-9876 monosuccinate) inhibits SYK activity in platelets via the glycoprotein VI (GPVI) receptor without prolonging bleeding time (BT) in monkeys or humans .
PF-915275 is a potent, selective and orally active human 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) inhibitor with a Ki of 2.3 nM and an EC50 of 15 nM (in HEK293 cells). The dose-dependent effect of PF-915275 on conversion of cortisone to cortisol in primary human and monkey hepatocytes, with an EC50 of 20 and 100 nM, respectively .
PI3K/mTOR Inhibitor-13 sodium is an orally active dual inhibitor of phosphoinositol 3-kinase (PI3K) and mTOR kinase. PI3K/mTOR Inhibitor-13 sodium has potential applications in sexual diseases, solid tumor and idiopathic pulmonary fibrosis (IPF) .
Risankizumab (BI 655066) is a humanised IgG monoclonal antibody, targeting IL-23 p19 subunit (Kd <10 pM) and inhibiting IL-17 production induced by human IL-23 in mouse splenocytes (IC50 = 2 pM). Risankizumab can be used to research immunological and inflammatory disorders such as psoriasis vulgaris, psoriatic arthritis, generalized pustular psoriasis and erythrodermic psoriasis .
Etripamil (MSP-2017) is a short-acting, L-type calcium-channel antagonist. Etripamil inhibits calcium influx through slow calcium channels, thereby slowing AV node conduction and prolonging the AV node refractory period. Etripamil increases heart rate and decreases systolic blood pressure. Etripamil can be used in the study of paroxysmal supraventricular tachycardia (PSVT) .
Antileishmanial agent-17 is a coumarin hybrid compound with antileishmanial effects (IC50 <0.78 μM). Antileishmanial agent-17 is safe to normal VERO cells. Antileishmanial agent-17 binds to folate pathway enzymes pteridine reductase and DHFR-TS. And Antileishmanial agent-17 shows the most potent with IC50 value of 0.40 μM against promastigote and 0.68 μM against amastigote, respectivley.
Pozelimab (REGN3918) is a fully human IgG4 anti-C5 monoclonal antibody. Pozelimab binds to C5 and C5 variants with high affinity and blocks complement-mediated hemolysis. Pozelimab can be used for the research of complement-mediated diseases .
Imvotamab (IGM-2323) is a CD20 and CD3 bispecific IGM antibody with dual action mechanism. Imvotamab is used to induce physiological T cell activation to prevent over-stimulation and subsequent down-regulation of immune function. Imvotamab can be used for the study of B-cell malignant tumors, multiple myeloma (MM) and non-Hodgkin's lymphoma (NHL) .
PI3K/mTOR Inhibitor-13 is an orally active dual inhibitor of phosphoinositol 3-kinase (PI3K) and mTOR kinase. PI3K/mTOR Inhibitor-13 has potential applications in sexual diseases, solid tumor and idiopathic pulmonary fibrosis (IPF) .
Ubrogepant (Standard) is the analytical standard of Ubrogepant. This product is intended for research and analytical applications. Ubrogepant (MK-1602) is an orally active and selective antagonist of calcitonin gene-related peptide receptor (CGRP). Ubrogepant has high affinity for CGRP receptors in human and rhesus monkeys, and can effectively block the cAMP response stimulated by α-CGRP. Ubrogepant can be used in the study of acute migraine .
PF-04856264 is a potent and selective Nav1.7 inhibitor, with IC50s of 28, 131, 19, and 42 nM for human, mouse, cynomolgus monkey and dog Nav1.7, respectively. PF-04856264 has low potency against the rat Nav1.7 channel. PF-04856264 shows analgesic effect .
TC-1698 dihydrochloride is a selective α7 nicotinic acetylcholine receptors agonist with EC50 value of 0.16 μM and 0.46 μM for monkey α7 nicotinic receptor and human α7 nicotinic receptor, respectively. TC-1698 dihydrochloride improves memory and has neuroprotective effects. TC-1698 dihydrochloride can be used for Alzheimer's disease research .
Guselkumab is a recombinant human IgG1 monoclonal antibody against the IL-23p19 subunit. Guselkumab binds to human and cynomolgus monkey IL-23 with Kd values of 3.3 and 1.9 pmol/L, respectively. Guselkumab inhibits production of cytokines lying downstream of the IL-23 signaling pathway and can be used for psoriatic arthritis research .
TC-1698 is a selective α7 nicotinic acetylcholine receptors agonist with EC50 value of 0.16 μM and 0.46 μM for monkey α7 nicotinic receptor and human α7 nicotinic receptor, respectively. TC-1698 improves memory and has neuroprotective effects. TC-1698 can be used for Alzheimer's disease research .
GS-9822 is a potent antivira agent with nanomolar activity against wild-type HIV-1 viruses. GS-9822 potently inhibits the LEDGF/p75-integrase interaction with an IC50 of 0.07 μM. GS-9822 has high in vitro metabolic stability and favorable oral pharmacokinetic profiles with low systemic clearance in rats, dogs, and monkeys .
Relacatib (SB-462795) is a novel, potent, and orally active inhibitor of human cathepsins K, L, and V with Ki values of 41 pM, 68 pM, and 53 pM, respectively. Relacatib inhibits endogenous cathepsin K in situ in human osteoclasts and human osteoclast-mediated bone resorption with IC50 values of 45 nM and 70 nM, respectively. Relacatib inhibits bone resorption in vitro in human tissue as well as in cynomolgus monkeys in vivo .
BI 186908 is a selective and orally active MCH receptor 1 antagonist with an IC50 of 22 nM and a Ki of 14 nM. BI 186908 binds with comparably high affinity to the recombinant human, cynomolgus monkey (IC50 of 18 nM), dog (IC50 of 23 nM) and rat (IC50 of 18 nM) MCH-R1. BI 186908 can significantly reduce the body weight of diet-induced obese rats. BI 186908 can be used for the study of obesity .
Ogalvibart (C-135-LS) is a human anti-SARS-CoV-2 monoclonal antibody (IgG1 type). Ogalvibart binds to the spike (S) glycoprotein receptor-binding domain (RBD) of SARS-CoV-2. Ogalvibart in combination with C144LS (1:1 ratio) shows good preventive activity and can effectively block the development of COVID19 in a rhesus monkey disease model .
GNUV201 is a PD-1 inhibitor with cross-reactivity in humans, mice and monkeys, which effectively blocks the PD-1/PD-L1 interaction. GNUV201 activates T cells and restores their anti-tumor activity, effectively inducing tumor regression. GNUV201 can be used in the research of related diseases such as colorectal cancer, melanoma, pancreatic cancer and colon cancer .
Gentulizumab (Gensci-059) is a humanized IgG4 antibody that targets CD47. Gentulizumab displays strong binding to CD47 in both human and monkey, and effectively inhibits the CD47-SIRPα interaction. Gentulizumab exhibits a potent antitumor activity. The isotype control for Gentulizumab can refer to Human IgG4 (S228P) kappa, Isotype Control (HY-P99003) .
CCR6 inhibitor 1 is a potent and selective CCR6 inhibitor, with IC50s of 0.45 and 6 nM for monkey and human CCR6, much more selective at CCR6 over human CCR1 (IC50, > 30000 nM), and CCR7 (IC50, 9400 nM). CCR6 inhibitor 1 markedly blocks ERK phosphorylation. CCR6 inhibitor 1 is used in the research of autoimmune diseases and cancer .
15(S)-Latanoprost is an analog of latanoprost in which the hydroxyl at carbon 15 is inverted relative to latanoprost. The IC50 values for the free acid forms of latanoprost and 15(S)-latanoprost were determined to be 3.6 nM and 24 nM, respectively, in a FP receptor binding assay using the cat iris sphincter muscle. A 3 μg dose of 15(S)-latanoprost caused a 1 mmHg reduction of IOP in normotensive cynomolgus monkeys.
GMA-839 is a selective modulator of the γ-aminobutyric acid A receptor (GABAA) with an IC50 value of 230 nM. GMA-839 exhibits potent anxiolytic-like activity, demonstrating significant dose-dependent anxiolytic effects in animal models, with an effective oral dose of 1.6 mg/kg. Significant increases in punished responding were observed in squirrel monkeys and pigeons. GMA-839 shows promise for research in the field of anxiolytics .
JNJ-39758979 dihydrochloride is a selective, orally active, and high-affinity histamine 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 .
AMG133 peptide payload TFA is a GLP-1 analog agonist peptide. AMG133 peptide payload TFA potently activates GLP-1R and exhibits weight loss and metabolic improvement activities. AMG133 peptide payload TFA can be used for the synthesis of AMG 133 (HY-164535) .
SHR-2042 is a selective agonist of the GLP-1 receptor.SHR-2042 improves glycemic control by activating the GLP-1 receptor, enhancing insulin secretion and inhibiting glucagon secretion. SHR-2042 combined with sodium N-(8-[2-hydroxybenzoyl] amino) caprylate (SNAC) promotes monomerization through the formation of micelles and improves oral absorption efficiency .
Osavampator (TAK-653) is a AMPA receptor positive allosteric modulator. Osavampator selectively binds to AMPA-R in a glutamate-dependent manner and induces Ca2+ influx in hGluA1i CHO cells (EC50 = 3.3 μM). Osavampator improves learning and memory in many models. Osavampator is can be used for the research of depressive disorders .
Semorinemab (RG 6100) is an anti-Tau humanized IgG4 monoclonal antibody, targets the N-terminal portion of the Tau protein (amino acid residues 6-23). Semorinemab binds with human Tau with a Kd value of 3.8 nM. Semorinemab can be used for the research of Alzheimer's Disease .
LTGO-33 is a potent and selective voltage-gated sodium channel NaV1.8 inhibitor. LTGO-33 inhibits NaV1.8 in the nM potency range and exhibits over 600-fold selectivity against human NaV1.1-NaV1.7 and NaV1.9. LTGO-33 exhibits state-independent inhibition with similar potencies on channels in the closed and inactivated conformations. LTGO-33 inhibits native TTX-R NaV1.8 currents in non-human primate and human DRG neurons, where it reduces action potential firing. LTGO-33 can be used for pain disorders research .
Mirikizumab (LY3074828) is a humanized IgG4 monoclonal antibody that targets the p19 subunit of interleukin 23 (IL-23). Mirikizumab binds to human and monkeyIL-23 with high affinity, with Kd values of 21 pM and 55 pM, respectively. By inhibiting the binding of IL-23 to IL-23R, Mirikizumab modulates the immune response and holds potential for research in ulcerative colitis and Crohn's disease .
Ubrogepant-d5 (MK-1602-d5) is deuterium labeled Ubrogepant. Ubrogepant (MK-1602) is an orally active and selective antagonist of calcitonin gene-related peptide receptor (CGRP). Ubrogepant has high affinity for CGRP receptors in human and rhesus monkeys, and can effectively block the cAMP response stimulated by α-CGRP. Ubrogepant can be used in the study of acute migraine .
SKI2496 is an orally active GnRH receptor antagonist (IC50: 0.25 nM for hGnRHR, 13.2 nM for monkey GnRHR, 279.2 nM for rat GnRHR). SKI2496 blocks Ca 2+ flux with an IC50 value of 0.76 nM. SKI2496 inhibits ERK1/2 phosphorylation with an IC50 value of 2.6 nM. SKI2496 inhbits serum LH concentrations, and can be used for research of sex hormone-dependent disorders .
Givosiran (ALN-AS1) sodium is a small interfering RNA that targets hepatic aminolevulinate synthase 1 (ALAS1) messenger RNA. Givosiran sodium downregulates ALAS1 mRNA and prevents accumulation of neurotoxic δ-aminolevulinic acid (ALA) and porphobilinogen (PBG) levels. Givosiran sodium demonstrates potent inhibitory activity against ALAS1 in mouse, rat, and cynomolgus monkey models. Givosiran sodium can be used for the research of acute hepatic porphyria (AHP) .
Veledimex (INXN-1001), a synthetic analog of the insect molting hormone ecdysone, is an orally active activator ligand for a proprietary gene therapy promoter system. Veledimex can be used to activate certain genes using the ecdysone receptor (EcR)-based inducible gene regulation system, the RheoSwitch Therapeutic System (RTS). Veledimex can cross blood-brain barrier (BBB) in both orthotopic GL-261 mice and cynomolgus monkeys .
JNJ-39758979, a chemical probe, is a selective, orally active, and high-affinity histamine 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 .
REGN4659 is a fully human anti-CTLA-4 monoclonal antibody and IgG1 antibody. REGN4659 binds to the extracellular domain of human and monkey CTLA-4 with high affinity and specificity. REGN4659 blocks CTLA-4 interaction with CD80 and CD86 ligands. REGN4659 significantly suppresses MC38.Ova tumor growth in CTLA-4 knock-in mice .
Givosiran (ALN-AS1) is a small interfering RNA that targets hepatic aminolevulinate synthase 1 (ALAS1) messenger RNA. Givosiran downregulates ALAS1 mRNA and prevents accumulation of neurotoxic δ-aminolevulinic acid (ALA) and porphobilinogen (PBG) levels. Givosiran demonstrates potent inhibitory activity against ALAS1 in mouse, rat, and cynomolgus monkey models. Givosiran can be used for the research of acute hepatic porphyria (AHP) .
4-Hydroxymethylpyrazole is the primary metabolite of Fomepizole (HY-B0876) produced through hepatic oxidative metabolism. 4-Hydroxymethylpyrazole exhibits a plasma concentration that is positively correlated with the administered dosage of Fomepizole, and it demonstrates a relatively short half-life. 4-Hydroxymethylpyrazole demonstrates inhibitory effects on alcohol dehydrogenase (ADH) in both humans and monkeys, but its inhibition constant is significantly higher than that of Fomepizole, rendering its in vivo impact negligible .
JBSNF-000088 (6-Methoxynicotinamide), a analog of nicotinamide (NA), is a potent and orally active Nicotinamide N-methyltransferase (NNMT) inhibitor with IC50s of 1.8 µM, 2.8 µM, and 5.0 µM for human NNMT, monkey NNMT and mouse NNMT, respectively. JBSNF-000088 inhibits NNMT activity, reduces MNA levels and drives insulin sensitization, glucose modulation and body weight reduction in animal models of metabolic disease .
Guanfu base A is an antiarrhythmic alkaloid isolated from Aconitum coreanum and is a potent noncompetitive CYP2D6 inhibitor, with a Ki of 1.20 μM in human liver microsomes (HLMs) and a Ki of 0.37 μM for the human recombinant form (rCYP2D6). Guanfu base A is also a potent competitive inhibitor of CYP2D in monkey (Ki of 0.38 μM) and dog (Ki of 2.4 μM) microsomes . Guanfu base A also inhibits HERG channel current .
Spartalizumab is a humanized PD-1 IgG4 monoclonal antibody, with a Kd of 0.83 nM for human PD-1 and a Kd of 0.93 nM for cynomolgus monkeyPD-1. Spartalizumab binds to PD-1 and blocks its interaction with the ligands PD-L1 and PD-L2. Spartalizumab induces increased IFNγ release. Spartalizumab can be used in the research of anaplastic thyroid carcinoma (ATC) and neuroendocrine neoplasms (NENs) .
Ganciclovir triphosphate (GCV-TP) is a synthetic 2'-deoxyguanosine analog with activity in inhibiting human cytomegalovirus (CMV) replication. Ganciclovir triphosphate is effective against CMV infection by binding to viral DNA polymerase and interfering with viral DNA synthesis. Ganciclovir triphosphate has an IC50 of 0.01 μM against CMV strains from humans, monkeys, mice, and guinea pigs. Ganciclovir triphosphate has also been used in gene-directed enzyme prodrug inhibition for cancer inhibition .
ALS-I-41 is a novel, potent and selective oxytocin receptor antagonist with the potential to modulate biological activities related to social behavior and mental disorders. ALS-I-41 is being evaluated for behavioral pharmacology experiments in non-human primates and can be administered via intranasal or intramuscular injection. The central nervous system penetration and metabolic rate of ALS-I-41 were studied by mass spectrometry analysis in cerebrospinal fluid and plasma of macaque monkeys .
Tanruprubart (ANX005) is a C1q inhibitor and C1q depleter. Tanruprubart is a human antibody expressed in CHO cells, with huIgG1 heavy chains and huκ light chains, and its predicted molecular weight (MW) is 145 kDa. For the isotype control of Tanruprubart, refer to Human IgG1 kappa, Isotype Control (HY-P99001). The IC50 of Tanruprubart is 346 ng/mL for humans and 259 ng/mL for rats; its EC50 is 3.8 ng/mL for humans, 5.2 ng/mL for rats, and 9.9 ng/mL for mice. Tanruprubart is applicable to the research of Guillain-Barré syndrome and Alzheimer's disease .
COX-1 ligand 1 (Compound 44) is a selective COX-1 ligand (Kds or Kis: 22 nM for rhesus monkey COX-1; 43 nM for hCOX-1). COX-1 ligand 1 inhibits [ 3H]PS13 binding to human COX-1. COX-1 ligand 1, when radiolabeled with 11C or 18F, can be used in studies of COX-1 imaging and psychiatric disorders .
PF-915275 (Standard) is the analytical standard of PF-915275. This product is intended for research and analytical applications. PF-915275 is a potent, selective and orally active human 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) inhibitor with a Ki of 2.3 nM and an EC50 of 15 nM (in HEK293 cells). The dose-dependent effect of PF-915275 on conversion of cortisone to cortisol in primary human and monkey hepatocytes, with an EC50 of 20 and 100 nM, respectively .
Ambenoxan hydrochloride is a central nervous system-acting skeletal muscle relaxant that is effective in mice, rats, rabbits, dogs, and monkeys without loss of the righting reflex. It has no peripheral neuromuscular blocking effects and significantly reduces or eliminates decerebrate rigidity in rabbits, but does not antagonize the effects of strychnine, leptazol, or tremorine. Like other central nervous system depressants, ambenoxan prolongs sleep duration with hexobarbitone, but it has no local anesthetic effects. In anesthetized cats, the agent lowers blood pressure and reduces the pressor response to epinephrine, but has no effect on norepinephrine.
ISIS 104838 sodium is an antisense oligonucleotide targeting TNF-α. ISIS 104838 sodium specifically binds to human TNF-α mRNA via Watson-Crick base pairing to form a DNA:RNA hybrid duplex, thereby recruiting the ubiquitously expressed intracellular enzyme RNase H to degrade the target mRNA and inhibit TNF-α protein synthesis at the transcriptional level. ISIS 104838 sodium induces moderate, self-limiting thrombocytopenia in cynomolgus monkeys. ISIS 104838 sodium can be used for the study of inflammatory diseases .
5-Hydroxy saxagliptin- 13C,d2-2 hydrochloride is the 13C- and deuterium labeled 5-Hydroxy saxagliptin hydrochloride. 5-Hydroxy saxagliptin hydrochloride is an active metabolite of Saxagliptin (HY-10285) and a potent and selective DPP-4 inhibitor. 5-Hydroxy saxagliptin hydrochloride has Ki values of 2.6 nM and 2.9 nM for humans and cynomolgus monkeys, respectively. 5-Hydroxy saxagliptin hydrochloride can be used in the research of type 2 diabetes mellitus .
Ganciclovir triphosphate (GCV-TP) disodium is a synthetic 2'-deoxyguanosine analog with activity in inhibiting human cytomegalovirus (CMV) replication. Ganciclovir triphosphate disodium is effective against CMV infection by binding to viral DNA polymerase and interfering with viral DNA synthesis. Ganciclovir triphosphate disodium has an IC50 of 0.01 μM against CMV strains from humans, monkeys, mice, and guinea pigs. Ganciclovir triphosphate disodium has also been used in gene-directed enzyme prodrug inhibition for cancer inhibition .
Ambenoxan is a central nervous system-acting skeletal muscle relaxant that is effective in mice, rats, rabbits, dogs, and monkeys without loss of the righting reflex. It has no peripheral neuromuscular blocking effects and significantly reduces or eliminates decerebrate rigidity in rabbits, but does not antagonize the effects of strychnine, leptazol, or tremorine. Like other central nervous system depressants, ambenoxan prolongs sleep duration with hexobarbitone, but it has no local anesthetic effects. In anesthetized cats, the agent lowers blood pressure and reduces the pressor response to epinephrine, but has no effect on norepinephrine.
Relugolix (TAK-385)?is a potent, orally active, nonpeptidic gonadotropin-releasing hormone (GnRH) antagonist. Relugolix possesses high affinity 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 .
INU-101 is a potent, selective and orally active 11β-hydroxysteroid dehydrogenase (11β-HSD) type 1 inhibitor. INU-101 has highly potent inhibitory activity in mouse, monkey and human 11β-HSD1, derived from liver microsomes. INU-101 can enhance insulin sensitivity and lower the fasting blood glucose level. INU-101 can be used for the research of metabolic disease, such as diabetes .
7-Ethoxycoumarin (Standard) is the analytical standard of 7-Ethoxycoumarin. This product is intended for research and analytical applications. 7-Ethoxycoumarin is a substrate of cytochrome P450 (CYP450). 7-Ethoxycoumarin has been used for the functional characterization of various CYPs and for the generation of 7-hydroxycoumarin (HY-N0573) .
Suvizumab (KD-247) is an neutralizing antibody anti-HIV-1. Suvizumab effectively neutralizes HIV-1MN, HIV-1SF2 and HIV-189.6 with IC50 values of 0.1 µg/mL, 1.0 µg/mL and 0.2 µg/mL, respectively. Suvizumab reduces the viral load of HIV. Suvizumab has good tolerance and can be used to prevent HIV infection .
7-Ethoxycoumarin is a substrate of cytochrome P450 (CYP450). 7-Ethoxycoumarin has been used for the functional characterization of various CYPs and for the generation of 7-hydroxycoumarin (HY-N0573) .
BMS-181885 is a selective 5-HT1 receptor agonist and a ligand for 5-HT1B/1D receptors. BMS-181885 exhibits anti-migraine activity. BMS-181885 can be used in the research of neurological diseases such as migraine .
RG-7152 is a tetrazolyl-substituted leukotriene D4 receptor antagonist that can induce peroxisomal β-oxidation and peroxisome bifunctional enzymes (PBEs) in hepatocytes in various animal models. It has been shown to significantly increase PBE levels and β-oxidation activity in rat and mouse liver homogenates, while smaller effects were observed in guinea pigs and monkeys and no effect in dogs. In vitro studies have also shown that it can induce PBEs comparable to clofibric acid, indicating its potential as a peroxisome proliferator .
4-Hydroxymethylpyrazole (Standard) is an analytical standard for 4-Hydroxymethylpyrazole (HY-33914). This product is intended for research and analytical applications. 4-Hydroxymethylpyrazole is the primary metabolite of fomepizole (HY-B0876) via hepatic oxidative metabolism. 4-Hydroxymethylpyrazole exhibits a plasma concentration that is positively correlated with the administered dosage of Fomepizole, and it demonstrates a relatively short half-life. 4-Hydroxymethylpyrazole inhibits alcohol dehydrogenase (ADH) in humans and monkeys, but the inhibition constant is much higher than that of fomepizole and is therefore negligible in vivo
CP-615003 is a potent and subtype-selective partial agonist of GABAA receptor (GABAA receptor) (Ki = 1.1 μM). CP-615003 is mainly converted into the active metabolite CP-900725 through oxidative deamination in monkeys and humans, and the latter also has GABAA receptor affinity. CP-615003 is a substrate of P-glycoprotein (P-gp/MDR1), resulting in severe limitation of its penetration into the central nervous system (CNS). CP-615003 can be used for the study of CNS-related indications .
Relacatib (Standard) is the analytical standard of Relacatib (HY-10294). This product is intended for research and analytical applications. Relacatib (SB-462795) is a novel, potent, and orally active inhibitor of human cathepsins K, L, and V with Ki values of 41 pM, 68 pM, and 53 pM, respectively. Relacatib inhibits endogenous cathepsin K in situ in human osteoclasts and human osteoclast-mediated bone resorption with IC50 values of 45 nM and 70 nM, respectively. Relacatib inhibits bone resorption in vitro in human tissue as well as in cynomolgus monkeys in vivo .
Relugolix-d6 is deuterium labeled Relugolix. Relugolix (TAK-385)?is a potent, orally active, nonpeptidic gonadotropin-releasing hormone (GnRH) antagonist. Relugolix possesses high affinity 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 .
SB-657510 (Standard) is the analytical standard of SB-657510 (HY-10656). This product is intended for research and analytical applications. SB-657510 is a selective urotensin II (UII) receptor (UT) antagonist. The Ki values are 61, 17, 30, 65 and 56 nM for human, monkey, cat, rat and mouse receptors, respectively. SB-657510 exerts anti-inflammatory effects by inhibiting UII-induced upregulation of inflammatory mediators such as adhesion molecules, cytokines, and tissue factor in human vascular endothelial cells .
Margetuximab (MGAH22) is a chimeric anti-HER2 monoclonal antibody optimized Fc domain, with an EC50 value of 39.33 ng/mL. Margetuximab can be used for researching metastatic HER2-positive breast cancer .
Cholesteryl oleate is an ester compound formed from Cholesterol (HY-N0322) and Oleic acid (HY-N1446), which is involved in lipid transport, storage and cell membrane formation in living organisms. Cholesteryl oleate may serve as a potential biomarker for prostate cancer. Cholesteryl oleate can also prepare cationic solid lipid nanoparticles (SLNs) for efficient gene silencing .
GSK3739936 (BMS-986180) is a potent HIV-1 allosteric integrase inhibitor with an IC50 value of 11.1 nM and an EC50 value of 1.7 nM. GSK3739936 is also a weak CYP inhibitor (IC50>24.3 μM). GSK3739936 shows favorable pharmacokinetic property in preclinical species with rapid absorption, low to moderate clearance and excellent oral bioavailability .
Iscalimab (CFZ-533) is a non-depleting IGg1 monoclonal antibody targeting CD40 (KD: 0.3 nM). Iscalimab can be used for research of Graves' hyperthyroidism and autoimmune diseases .
Lanadelumab (SHP643) is a human IgG1 monoclonal antibody against plasma kallikrein (pKal) with an Ki value of 0.12 nM. Lanadelumab inhibits both free and HMWK (high molecular weight kininogen)-bound pKal. Lanadelumab has the potential for the research of hereditary angioedema .
LY3541860 is a selective anti-CD19 antibody that both binds human CD19 with high affinity and selectively binds human B cells (Kd values: 76.8 pM and 94.5 nM for humans and cynomolgus monkeys, respectively). LY3541860 inhibits CpG-induced CD69 expression (IC50 = 0.006 nM). LY3541860 exhibits potent B cell inhibitory activities. LY3541860 can inhibit both BCR- and TLR-induced human B cell activation. LY3541860 can be used for the research of autoimmune diseases .
15(S)-Latanoprost (Standard) is the analytical standard of 15(S)-Latanoprost. This product is intended for research and analytical applications. 15(S)-Latanoprost is an analog of latanoprost in which the hydroxyl at carbon 15 is inverted relative to latanoprost. The IC50 values for the free acid forms of latanoprost and 15(S)-latanoprost were determined to be 3.6 nM and 24 nM, respectively, in a FP receptor binding assay using the cat iris sphincter muscle. A 3 μg dose of 15(S)-latanoprost caused a 1 mmHg reduction of IOP in normotensive cynomolgus monkeys.
Relugolix (Standard) is the analytical standard of Relugolix. This product is intended for research and analytical applications. Relugolix (TAK-385) is a potent, orally active, nonpeptidic gonadotropin-releasing hormone (GnRH) antagonist. Relugolix possesses high affinity 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 .
CT-996 is an orally active GLP-1RA agonist with an EC50 of 0.49 nM. CT-996 reduces the recruitment of β-arrestin and the internalization of GLP-1R. CT-996 suppresses postprandial blood glucose in mice expressing human GLP-1 receptors and enhances glucose-stimulated insulin secretion (GSIS) in obese monkeys during intravenous glucose challenge. CT-996 can be used for the research of type 2 diabetes (T2D) and obesity .
LY86057 is an ergoline derivative without N1 substituents. It has higher affinity for porcine, squirrel monkey and human 5-HT2 receptors than rats and is an antagonist of 5-HT2 receptors. When studying the differences in recognition of a series of ergolines between species, LY86057 was found to be more selective for 5-HT2 receptors. Compared with LY53857, LY108742 resulted in a higher affinity for rat 5-HT2 receptors even when the N1 substituent was only methyl.
ARI-3099 is an oral fibroblast activation protein (FAP) inhibitor. ARI-3099 specifically inhibits the proteolytic activity of FAP and blocks the cleavage of human FGF-21 between residues P171 and S172. ARI-3099 extends the half-life of circulating human FGF-21 in mice. ARI-3099 can be used in the research of type 2 diabetes and metabolic disorders .
JNJ-39758979 (Standard) is the analytical standard of JNJ-39758979 (HY-101189). This product is intended for research and analytical applications. JNJ-39758979, a chemical probe, is a selective, orally active, and high-affinity histamine 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 .
Onartuzumab (MetMAb) is a unique, humanized and affinity-matured monovalent (one-armed) monoclonal antibody against the MET receptor. Onartuzumab potently inhibits HGF binding and receptor phosphorylation and signaling. Onartuzumab has antibody-like pharmacokinetics and antitumor activity .
Bofanglutide (GZR18) is an analog of glucagon-like peptide-1 (GLP-1), which exhibits agonistic activity for GLP-1 receptor, with an EC50 of 0.677 nM. GZR18 ameliorates type 2 diabetes .
SB-267268 is a selective and nonpeptidic alpha(v)beta3 (αvβ3) and alpha(v)beta5 (αvβ5) integrins antagonist, with Kis of 0.9, 0.5 and 0.7 nM for human αvβ3, monkey αvβ3 and human αvβ5, respectively. SB-267268 inhibits human and mouse αvβ3 with IC50s of 0.68 and 0.29 nM, respectively. SB-267268 reduces angiogenesis and VEGF expression .
JBSNF-00002 is an orally active small molecule inhibitor of the tricyclic nicotinamide N-methyltransferase (NNMT) with IC50 values for human, mouse and monkey sources of NNMT of 33, 210 and 190 nM respectively. JBSNF-00002 can reduce endogenous MNA levels in U2OS osteosarcoma cells, with its EC50 being 2.5 μM. JBSNF-00002 exhibits significant anti-obesity and anti-diabetic activities in the diet-induced obesity (DIO) model. JBSNF-00002 can be used for the study of metabolic diseases such as obesity, type 2 diabetes and non-alcoholic fatty liver disease .
JBSNF-00002 hydrochloride is an orally active small molecule inhibitor of the tricyclic nicotinamide N-methyltransferase (NNMT) with IC50 values for human, mouse and monkey sources of NNMT of 33, 210 and 190 nM respectively. JBSNF-00002 hydrochloride can reduce endogenous MNA levels in U2OS osteosarcoma cells, with its EC50 being 2.5 μM. JBSNF-00002 hydrochloride exhibits significant anti-obesity and anti-diabetic activities in the diet-induced obesity (DIO) model. JBSNF-00002 hydrochloride can be used for the study of metabolic diseases such as obesity, type 2 diabetes and non-alcoholic fatty liver disease .
DA-302168S is an orally active and selective agonist targeting the GLP-1R, with EC50 value of 1.32 nM. DA-302168S stimulates insulin secretion and shows hypoglycemic effects. DA-302168S decreases food intake. DA-302168S mainly activates GLP-1R of monkeys and humans, and exhibits little excitatory effect on GLP-1R of rats, mice, and dogs. DA-302168S can be used for type 2 diabetes and obesity study .
VL-422 is an ionizable cationic lipid. VL-422 delivers CRISPR complementary single-guide RNA (sgRNA) and Cas9 mRNA to enable in vitro and in vivo gene editing. LNPs containing VL-422 loaded with Cas9 mRNA and sgRNA targeting the ANGPTL3 gene induce the deletion of premature stop codons within the ANGPTL3 gene in the liver of cynomolgus monkeys. Loss-of-function of ANGPTL3 leads to decreased levels of LDL, HDL and cholesterol in plasma. The VL-422 delivery system can be used for the research of gene editing strategies targeting lipid metabolism diseases .
Navivumab (CT-P23) is a monoclonal antibody targeting the hemagglutinin (HA) of influenza A virus. Navivumab binds to the HA2 stem fusion domain and the low-variability HA2 region of influenza viruses. Navivumab neutralizes influenza A viruses of subtypes H1, H2, H5, and H9. Navivumab is applicable to research related to influenza and influenza A .
AS3288802, a highly selective active plasminogen activator inhibitor-1 (PAI-1) antibody, is a PAI-1 inhibitor with a human IC50 and EC50 values of 4.2 ng/mL. AS3288802 can be used for the research of thrombosis and fibrosis-related diseases .
Cudarolimab (IBI101) is a completely human anti-OX40 (CD134, a co stimulating molecule expressed by activated immune cells) antibody. Cudarolimab inhibits the binding of OX40 to its ligand OX40L. Cudarolimab has antitumor activity and can be used in cancer related research .
Digitoxin (Standard) is the analytical standard of Digitoxin. This product is intended for research and analytical applications. Digitoxin is an anti-cancer agent. Digitoxin induces apoptosis, inhibits influenza cytokine storm, causes DNA double-stranded breaks (DSBs) and blocks the cell cycle at the G2/M phase. Digitoxin induces calcium uptake into cells by forming transmembrane calcium channels and can be used for research of heart failure .
Digitoxin is an anti-cancer agent. Digitoxin induces apoptosis, inhibits influenza cytokine storm, causes DNA double-stranded breaks (DSBs) and blocks the cell cycle at the G2/M phase. Digitoxin induces calcium uptake into cells by forming transmembrane calcium channels and can be used for research of heart failure .
Prezalumab (AMG 557) is a humanized IgG2 monoclonal antibody targeting ICOSL. Prezalumab inhibits T cell activation and related immune responses by binding to ICOSL and blocking the interaction between ICOS and ICOSL. Prezalumab can be used in the research of autoimmune diseases and inflammatory diseases such as systemic lupus erythematosus. Recommend Isotype Controls: Human IgG2 kappa, Isotype Control (HY-P99002) .
TP0463518 is an orally active, competitive pan-inhibitor of hypoxia-inducible factor prolyl hydroxylases PHD1/2/3. TP0463518 competitively inhibits human PHD1 (IC50=18 nM), PHD2 (Ki=5.3 nM), and PHD3 (IC50=63 nM), and targets monkeyPHD2 with an IC50 of 22 nM. TP0463518 inhibits PHD-catalyzed hydroxylation to stabilize HIFα, thereby upregulating erythropoietin (EPO) expression and enhancing intestinal iron absorption (such as increased DMT-1 and dCYTb expression), improving anemia. TP0463518 is mainly used for the research of renal anemia and inflammatory anemia .
A-86929 is a highly potent and selective dopamine D1 receptor agonist with a pKi value of 7.3. In the 6-OHDA (HY-B1081)-induced unilateral nigrostriatal lesion rat model, A-86929 significantly induces rotational behavior. It also improves motor function in the MPTP (HY-15608)-induced Parkinson's disease marmoset model. Additionally, A-86929 demonstrates potential therapeutic value in reducing cocaine-seeking behavior in rats and reversing Haloperidol (HY-14538)-induced cognitive deficits in rhesus monkeys. A-86929 can be used for research in neurological disorders .
AMG-424 (XmAb968) is a human bispecific antibody (bsAb) targeting CD38 & CD3E. AMG-424 kills CD38-expressing cancer cells, triggers T-cell proliferation and attenuates cytokine release. AMG 424 has antitumor activity in a bone marrow-invasive mouse cancer model and induces peripheral B-cell depletion in cynomolgus monkeys. AMG-424 can be used in multiple myeloma research. Recommended isotype control: half-IG G1-kappa/(scFv-heavy-lambda)-h-CH2-CH3 .
JBSNF-00002 TFA is an orally active small molecule inhibitor of the tricyclic nicotinamide N-methyltransferase (NNMT) with IC50 values for human, mouse and monkey sources of NNMT of 33, 210 and 190 nM respectively. JBSNF-00002 TFA can reduce endogenous MNA levels in U2OS osteosarcoma cells, with its EC50 being 2.5 μM. JBSNF-00002 TFA exhibits significant anti-obesity and anti-diabetic activities in the diet-induced obesity (DIO) model. JBSNF-00002 TFA can be used for the study of metabolic diseases such as obesity, type 2 diabetes and non-alcoholic fatty liver disease .
L-771688 hydrochloride is a potent and highly selective α1A-adrenoceptor antagonist (Kd=43-90 pM). L-771688 hydrochloride is effective against cloned human, rat and dog α1A-adrenergic receptors. L-771688 exhibits high affinity (Ki ≤ 1 nM) and over 500-fold selectivity over the α1B and α1D isoforms. L-771688 potently antagonizes norepinephrine-induced responses at these receptors. Inhibits contractions induced by phenylephrine or A-61603 in rat, dog, human and monkey models .
MK 0686, a potent bradykinin B1 receptor antagonist, demonstrates autoinduction of metabolism in rhesus monkeys after oral administration. It undergoes significant biotransformation primarily via oxidation pathways, leading to the formation of metabolites like M11 and M13 in rhesus liver microsomes. This metabolic induction is mediated by CYP2C75, as evidenced by increased mRNA expression, protein levels, and catalytic activity of this enzyme in hepatocytes and liver microsomes from MK 0686-treated animals. The autoinduction phenomenon suggests that MK 0686 enhances its own metabolism by upregulating CYP2C75, potentially influencing its systemic exposure and pharmacokinetics over time .
Stapokibart (CM310) is a humanized monoclonal antibody targeting IL-4Rα (KD values of 0.25 nM, 1.50 nM, and 2.75 nM for human, cynomolgus monkey, and rat IL-4Rα, respectively). Stapokibart effectively blocks the interaction of cytokines IL-4 and IL-13 with their co-receptor subunit IL-4Rα. Stapokibart reduces IL-4 and IL-13 mRNA, inhibits CD23 upregulation, and inhibits IL-4 and IL-13-induced STAT6 activation. Stapokibart improves inflammation (airway inflammation, rhinitis, dermatitis) .
Atiprosine (AY-28228) is an orally effective selective α1-adrenergic receptor antagonist with a pA2 value of 8.11. Atiprosine exhibits antagonistic activity against α2-adrenergic receptors (α1-adrenergic receptor), 5-HT₂ receptors (5-HT₂ receptor), and H₁ receptors (H₁ receptor). The pA2 values for these receptors are 6.04, 6.87, and 7.32 respectively. Atiprosine has antihypertensive and hypotensive effects in rats, dogs, and monkeys. It can be used for research on cardiovascular and mental disorders.
Avosentan (Standard) is the analytical standard of Avosentan (HY-15195). This product is intended for research and analytical applications. Avosentan is an orally active endothelin (ETA) receptor antagonist. Avosentan can block the ETA receptor, thereby reducing vascular contraction, and exerting a renal protective effect. Avosentan inhibits vascular contraction caused by ET-1 and alleviates the reduction in retinal and optic nerve head blood flow induced by it, lowering intraocular pressure in the glaucoma monkey model. Avosentan non-specifically blocks ETB receptors at high doses, inhibiting ETB-mediated diuresis and natriuresis, and may cause fluid retention. Avosentan can be used to reduce proteinuria with diabetic nephropathy, but induces significant fluid overload and congestive heart failure.
JBSNF-00002 free base is an orally active small molecule inhibitor of the tricyclic nicotinamide N-methyltransferase (NNMT) with IC50 values for human, mouse and monkey sources of NNMT of 33, 210 and 190 nM respectively. JBSNF-00002 free base can reduce endogenous MNA levels in U2OS osteosarcoma cells, with its EC50 being 2.5 μM. JBSNF-00002 free base exhibits significant anti-obesity and anti-diabetic activities in the diet-induced obesity (DIO) model. JBSNF-00002 free base can be used for the study of metabolic diseases such as obesity, type 2 diabetes and non-alcoholic fatty liver disease .
AMG133 peptide payload is a GLP-1 analog agonist peptide. AMG133 peptide potently activates GLP-1R, and exhibits weight loss and metabolic improvement activities. AMG133 peptide payload can be used for the synthesis of AMG 133 (HY-164535) .
MORF-627 is a highly selective, orally active integrin αvβ6 inhibitor. By blocking TGF-β1 activation and pSMAD2 signaling, MORF-627 significantly reduces collagen deposition, epithelial-mesenchymal transition markers, and structural changes in fibrotic cells. MORF-627 exhibits significant antifibrotic efficacy without genotoxicity in idiopathic pulmonary fibrosis models. However, MORF-627 induces bladder epithelial proliferation and early invasive urothelial carcinoma in cynomolgus monkeys and human cells, and this toxic effect can be reversed by exogenous TGF-β. MORF-627 can be used for studying the pathological mechanisms of pulmonary fibrosis and evaluating drug safety .
GSK1842799, an alkyl-substituted biaryl amino alcohol, is a selective S1P1 modulator developed for multiple sclerosis (MS). Upon phosphorylation, GSK1842799-P exhibited subnanomolar S1P1 agonist activity with over 1000-fold selectivity over S1P3. The compound showed good oral bioavailability, rapid in vivo conversion to GSK1842799-P, and significant lymphocyte count reduction at 0.1 mg/kg. It matched FTY720 efficacy at 3 mg/kg in the mouse EAE model and achieved comparable plasma levels to FTY-720 phosphate in cynomolgus monkeys. With favorable ADME, PK/PD properties, and toxicology, GSK1842799 advanced to further clinical development .
A1480LS is a peripherally restricted, orally active covalent and irreversible inhibitor of DAGLα and DAGLβ, with IC50 values of 6 nM and 4 nM against human targets, respectively, and IC50 values ≤15 nM across mouse, rat, dog, monkey and human systems. A1480LS reduces the levels of 2-arachidonoylglycerol, arachidonic acid, and cyclooxygenase- and lipoxygenase-derived eicosanoids. A1480LS inhibits injury-induced production of 2-arachidonoylglycerol and arachidonic acid in the peripheral sciatic nerve, and suppresses the responses of high-threshold and wide-dynamic-range-like dorsal horn neurons to mechanical stimulation. A1480LS alleviates pain behaviors in rat models of inflammatory pain, neuropathic pain and chemotherapy-induced peripheral neuropathy .
15(R)-15-Methyl Prostaglandin F2α (15(R)-Carboprost; 15(R)-15-methyl PGF2α) is a metabolically stable analog of PGF2α. 15(R)-15-Methyl Prostaglandin F2α is an inactive, prodrug PGF agonist designed for activation by gastric acid after oral administration. Acid-catalyzed epimerization of 15(R)-15-Methyl Prostaglandin F2α converts it into the active 15(S)-isomer. The 15(S)-isomer induces luteolysis when injected in rhesus monkeys at a dose of about 12 mg/animal, while the 15(R)-isomer does not.
Glyceryl trinonanoate is a triacylglycerol containing nonanoic acid at the sn-1, sn-2 and sn-3 positions. It has been found in Schizochytrium biomass. 1 1,2,3-Trinonanoyl-rac-glycerol increases blood levels of the ketone body D-(-)-3-hydroxybutyrate in neonatal rhesus monkeys. 2|1. Mioso, R., Toledo Marante, FJ, González, JE, et al. Schizochytrium sp. metabolite analysis. Oleaginous microbial sources of biodiesel by GC-MS. braz. J. Microbiology. 45(2), 403-409 (2014).|2. Tetrick, MA, Greer, FR and Benevenga, NJ Blood D- ( )-3-Hydroxybutyric acid concentration. Compare. medicine. 60(6), 486-490 (2010).
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 high affinity 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 .
15-keto-17-phenyl trinor Prostaglandin F2α (15-keto-17-phenyl trinor PGF2α) is an F-series prostaglandin (PG) analog. The potential metabolite of 15-keto-17-phenyl trinor Prostaglandin F2α in animals is 15-keto PG. 15-keto PG can slightly reduce the intraocular pressure (1 mm Hg) in normal cynomolgus monkeys when administered at a dose of 1 μg/eye. 15-keto-17-phenyl trinor Prostaglandin F2α is a miotic agent in cats, reducing the pupil diameter by 8 mm at a dose of 5 μg/eye.
Pafuramidine (maleate) (DB289 (maleate)) is an orally active proagent of Furamidine (HY-110137A). Pafuramidine (maleate) (DB289 (maleate)) is a potent anti-parasitic agent, can be used to research trypanosomiasis, Pneumocystis pneumonia and malaria .
BAY-356, a potent TWEAK receptor agonist, is an aglycosylated anti-TWEAK receptor antibody. BAY-356 triggers TWEAKR hyperactivation, activates NFκB and STAT1 pathways, and undergoes TWEAKR-dependent internalization. BAY-356 can be used for the research of colorectal cancer, bladder cancer, non-small cell lung cancer and pancreatic cancer[1][2].
Molidustat (Standard) is the analytical standard of Molidustat. This product is intended for research and analytical applications. Molidustat (BAY 85-3934) is an orally active inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH) with IC50 values of 480 nM, 280 nM, and 450 nM for PHD1, PHD2, and PHD3, respectively. Molidustat can elevate the levels of circulating erythropoietin (EPO) to near-normal physiological ranges. Molidustat can be utilized in the research of renal anemia .
Iocarmic acid is a myelographic contrast agent. Iocarmic acid is used for lumbar nerve root angiography and ventriculography. Iocarmic acid induces arachnoiditis via lumbar subarachnoid injection. Iocarmic acid can be used for the research of arachnoiditis .
Inclacumab (Anti-Human selectin P Recombinant Antibody) is a human monoclonal IgG4 antibody selectively targets P-selectin with a Kd value of 9.9 nM. Inclacumab inhibits P-selectin glycoprotein ligand 1 (PSGL-1) mimetic peptide bind with P-selectin with an IC50 value of 1.9 μg/mL and strongly inhibits cell adhesion .
Pafuramidine (Standard) is the analytical standard of Pafuramidine. This product is intended for research and analytical applications. Pafuramidine (DB289) is an orally active proagent of Furamidine (HY-110137A). Pafuramidine is a potent anti-parasitic agent, can be used to research trypanosomiasis, Pneumocystis pneumonia and malaria .
Molidustat sodium is an orally active inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH) with IC50 values of 480 nM, 280 nM, and 450 nM for PHD1, PHD2, and PHD3, respectively. Molidustat sodium can elevate the levels of circulating erythropoietin (EPO) to near-normal physiological ranges. Molidustat sodium can be utilized in the research of renal anemia .
Pafuramidine (DB289) is an orally active proagent of Furamidine (HY-110137A). Pafuramidine is a potent anti-parasitic agent, can be used to research trypanosomiasis, Pneumocystis pneumonia and malaria .
Molidustat (BAY 85-3934) is an orally active inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH) with IC50 values of 480 nM, 280 nM, and 450 nM for PHD1, PHD2, and PHD3, respectively. Molidustat can elevate the levels of circulating erythropoietin (EPO) to near-normal physiological ranges. Molidustat can be utilized in the research of renal anemia .
Diflorasone is a potent topical anti-inflammatory Corticosteroid. Diflorasone induces vasoconstriction when applied topically. Diflorasone can be used in research related to psoriasis, atopic dermatitis/neurodermatitis .
KHK2840 is a potent CD40 agonist with a Kd value of 0.485 nM for hCD40. KHK2840 delivers agonistic signals in tumor-bearing hCD40 transgenic mice and human peripheral blood B cells. KHK2840 upregulates CD80, CD86, CD95 and IL-12p70 expression. KHK2840 enhances antitumor efficacy of anti-PD-1 antibody and Paclitaxel (HY-B0015). KHK2840 can be used for the research of cancer, such as colon cancer and melanoma .
Trecovirsen is an antiviral agent targeting HIV gag mRNA, which hybridizes with complementary HIV gag mRNA at the initiation site. Trecovirsen induces a reversible, dose-dependent prolongation of activated partial thromboplastin time via its polyanionic properties. Trecovirsen is applicable to research related to HIV infection .
15-keto Latanoprost is a potential metabolite of latanoprost (HY-B0577) when administered to animals. 15-keto Latanoprost is also one of the common minor impurities found in commercial preparations of the bulk drug compound. Although much less potent that the parent compound latanoprost, 15-keto latanoprost still retains the ability to produce a small but measurable decrease (1 mm Hg) in the intraocular pressure of normal cynomolgus monkeys when administered at a dose of 1 μg/eye.1 15-keto Latanoprost is also a miotic in the normal cat eye, causing an 8 mm Hg reduction in pupillary diameter at 5 μg/eye. Again, this is not as potent as many other F-type prostaglandins; for example, prostaglandin F2α will produce this degree of miosis at a dose of less than 1 μg/eye.
dWIZ-1 is an orally active molecular glue and chemical probe targeting the WIZ transcription factor, which based on an IMiD backbone, binding to human WIZ with an affinity of 3.5 μM. dWIZ-1 recruits WIZ to the cereblon-DDB1 complex via its ZF7 domain, thereby triggering proteasome-dependent degradation of WIZ. dWIZ-1 significantly induces fetal hemoglobin expression in erythroblasts while reducing the level of inhibitory H3K9 dimethylation at WIZ binding sites such as the β-globin locus. Meanwhile, dWIZ-1 does not affect the proliferation and differentiation of erythroblasts, and no cytotoxicity is observed in in vitro cells or cynomolgus monkey models. dWIZ-1 serves as a critical tool molecule for investigating the mechanism and underlying pathways of sickle cell disease .
Anti-EphA2 Antibody (1C1) (MEDI-547 antibody) is an anti-EphA2 monoclonal antibody. Anti-EphA2 Antibody (1C1) can induce degradation of EphA2 protein. Anti-EphA2 Antibody (1C1) conjugated with McMMAF (HY-15578) can form an antibody-conjugated drugs, which has potent antitumor activity. Anti-EphA2 Antibody (1C1) can be used for the research of cancer, such as prostate cancer and glioma .
Rugonersen (RG6091; RO7248824) is a locked-nucleic acid (LNA)- modified antisense oligonucleotides (ASOs), and results in reduction of ubiquitin-protein ligase E3A (UBE3A) silencing. Angelman syndrome (AS) is a severe neurodevelopmental disorder caused by the loss of neuronal E3 ligase UBE3A, Rugonersen has been used for AS reasearch .
Rugonersen sodium is a locked-nucleic acid (LNA)- modified antisense oligonucleotides (ASOs), and results in reduction of ubiquitin-protein ligase E3A (UBE3A) silencing. Angelman syndrome (AS) sodium is a severe neurodevelopmental disorder caused by the loss of neuronal E3 ligase UBE3A, Rugonersen has been used for AS reasearch .
LRRK2-IN-4 is a potent, selective, CNS-penetran and orally active leucine-rich repeat kinase 2 (LRRK2) inhobitor with an IC50 of 2.6 nM. LRRK2-IN-4 has the potential for the research of Parkinson’s disease .
Zigakibart (BION-1301) is an IgG4-kappa, humanized monoclonal antibody against TNFSF13 (tumor necrosis factor (TNF) superfamily member 13, APRIL, CD256). Zigakibart exhibits anti-inflammatory activity .
NGM-438 is a humanized monoclonal antibody antagonist of LAIR1, with a Ka of 0.26 nM for human LAIR1 and 4.28 nM for cynomolgus monkeyLAIR1. NGM-438 blocks the binding of LAIR1 to its Collagen ligand and antagonizes the Collagen-induced LAIR1 signaling pathway. NGM-438 reverses FcγR signaling inhibition in myeloid cells, induces dendritic cells to secrete TNFα, promotes T cell proliferation, and triggers myeloid inflammation and allogeneic T cell responses. NGM-438 sensitizes refractory mouse lung cancer to PD-1 blockade, increases the content of intratumoral CD8 + T cells and the expression of inflammatory genes. NGM-438 is applicable to research related to solid tumors, refractory solid tumors and non-small cell lung cancer .
Quinpirole (LY 171555; (-)-LY 141865) is a D2/D3dopamine receptor agonist and a CaV1.3 calcium channel modulator. Quinpirole normalizes dendritic spine density in dopamine-depleted striatum, upregulates the protein expression of BCL2 and GluR2, downregulates the protein expression of BAX, and delays the onset of seizures. Quinpirole enhances learning and memory, inhibits neuronal apoptosis (apoptosis), and induces anxiety-like, stereotyped, and compulsive behaviors. Quinpirole disrupts prepulse inhibition in rhesus monkeys, enhances the activity of paraventricular thalamic neurons to promote recovery from Isoflurane anesthesia, and alters the composition of the gut microbiota in rats. Quinpirole can be used in research related to dyskinesia, pain, epilepsy, and neurological disorders including anxiety disorder, obsessive-compulsive disorder, and schizophrenia .
QX008N is a humanized IgG1 monoclonal antibody and also a TSLP inhibitor with a KD value of 0.0175 nM. QX008N blocks TSLP-induced signaling pathways by inhibiting the interaction of TSLP-TSLPR-IL-7Rα. QX008N reduces eosinophil and IgE levels, improves pulmonary function, blocks TSLP-induced inflammation, and enhances the inhibitory effect on inflammatory mediators when administered in combination with anti-IL-4R antibodies. QX008N is applicable to relevant research on asthma .
Irdabisant (CEP-26401) hydrochloride is a selective, orally active and blood-brain barrier (BBB) penetrant histamine H3 receptor (H3R) inverse agonist/inverse agonist with Ki values of 7.2 nM and 2.0 nM for rat H3R and human H3R, respectively. Irdabisant hydrochloride has relatively low inhibitory activity against hERG current with an IC50 of 13.8 μM. Irdabisant hydrochloride has cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant hydrochloride can be used to research schizophrenia or cognitive impairment .
BGT-002 (326E) is an orally active dual ACLY inhibitor and PPARα agonist. BGT-002 reduces lipogenesis by inhibiting synthesis and promoting efflux. BGT-002 demonstrates efficacy in ameliorating metabolic dysfunction-associated steatohepatitis (MASH) and improving hyperlipidemia in vivo. BGT-002 can be used for hypercholesterolemia and MASH research .
Irdabisant (CEP-26401) is a selective, orally active and blood-brain barrier (BBB) penetrant histamine H3 receptor (H3R) inverse agonist/inverse agonist with Ki values of 7.2 nM and 2.0 nM for rat H3R and human H3R, respectively. Irdabisant has relatively low inhibitory activity against hERG current with an IC50 of 13.8 μM. Irdabisant has cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant can be used to research schizophrenia or cognitive impairment .
Alentemol (hydrobromide) is a dopamine antagonist and dihydrophenalene analog with dimethylamino substitution and an orthophenolic hydroxy group relative to the amino nitrogen. Alentemol (hydrobromide) does not impair escape response at a dose that completely suppresses conditioned avoidance in rats .
L-Alanyl-L-leucine is a competitive inhibitor of small intestinal glycyl-L-leucine hydrolase with Ki values of 0.53 mM (phosphate buffer) or 0.22 mM (Tris buffer). L-Alanyl-L-leucine can be used for research on Hartnup disease and cystinuria .
L-Alanyl-L-leucine is an endogenous metabolite. This product is used for research and analytical applications. L-Alanyl-L-leucine is a competitive inhibitor of small intestinal glycyl-L-leucine hydrolase with Ki values of 0.53 mM (phosphate buffer) or 0.22 mM (Tris buffer). L-Alanyl-L-leucine can be used for research on Hartnup disease and cystinuria .
Grisnilimab (WT1) is an IgG2a monoclonal antibody targeting CD7. Grisnilimab only binds to lymphoid tissues and T lymphocytes, with no off-target binding to normal tissues. Grisnilimab can be used to synthesize the immunotoxin WT1-SMPT-dgRTA, which exerts cytotoxic effects on T-lymphoblastic leukemia cells. Grisnilimab is applicable to relevant research on leukemia .
MK-3901 is a selective P2X3 receptor antagonist with an IC50 of 24 nM. MK-3901 inhibits UGT1A1 (with an IC50 of 1 μM) and CYP2C9 (with an IC50 of 5.7 μM). MK-3901 activates PXR. MK-3901 induces hyperbilirubinemia. MK-3901 can be used for the research of inflammatory pain .
MAO-B-IN-6 is a potent, selective and orally active MAO-B inhibitor with an IC50 of 0.019 µM. MAO-B-IN-6 shows more efficacious than Safinamide in vitro and in vivo. MAO-B-IN-6 has the potential for the research of parkinson's disease (PD) .
SHR-A1403 Antibody is an anti-c-Met monoclonal antibody. SHR-A1403 Antibody down-regulates phosphorylated c-Met, Akt, ERK, weakens intracellular signal cascades, and mediates antibody-c-Met complex endocytosis. SHR-A1403 Antibody can be used for the research of c-met-overexpressing cancers and pancreatic ductal adenocarcinoma .
U-11634 is an orally active dopamine β-hydroxylase noncompetitive inhibitor, with rat LD50 values of 1197 mg/kg (subcutaneous) and 524 mg/kg (oral). U-11634 blocks conversion of dopamine to norepinephrine and reduces norepinephrine levels in brain. U-11634 decreases food intake and spontaneous motor activity via dietary inclusion. U-11634 induces thyroid toxicity and inhibits pregnancy. U-11634 inhibits deciduomata formation in intact and steroid-treated rats, with no reversal by progesterone or oestradiol. U-11634 can be used for pregnancy .
Opugotamig olatansine (IMGN151) is a folate receptor alpha (FRα)-targeting antibody-drug conjugate (ADC). Opugotamig olatansine comprises antibody Opugotamig (HY-P990935) and linker-payload NMS-P945 (HY-185569). Opugotamig olatansine binds to two independent epitopes of FRα and promotes antibody binding, internalization, and processing. Opugotamig olatansine can be used for the research of FRα-positive ovarian cancer .
AGN-190851 is a potent and selective agonist of α2-adrenergic receptor (α2 adrenoceptor). AGN-190851 induces dose-dependent water diuresis in rats, and inhibits vasopressin V2 receptor in a species-dependent manner in vitro, thereby suppressing cAMP production. AGN-190851 enhances the contraction of porcine myometrium. AGN 190851 can be used in studies on renal diuretic mechanisms, pharmacology of α2-adrenergic receptor subtypes, and parturition .
Cubebin ((-)-Cubebin), a dibenzyl butyrolactone lignan, is an orally active AChE inhibitor. Cubebin binds to active sites of NF-κB, TNF-α, and TGF-β1 via hydrogen and hydrophobic interactions, obstructing critical residues to inhibit pro-inflammatory or renal fibrosis-related activity. Cubebin enhances p38 MAPK phosphorylation to increase tyrosinase gene expression, stimulating melanogenesis via elevated tyrosinase activity, expression, and mRNA levels. Cubebin reduces oxidative stress via enhanced endogenous antioxidant enzyme activity and inhibited lipid peroxidation, regulates lipid metabolism, improves glycemic control, and exerts renoprotective effects via reduced renal dysfunction markers and improved renal architecture. Cubebin shows antimicrobial activity. Cubebin exerts larvicidal activity against Angiostrongylus cantonensis larvae, with no cytotoxicity toward monkey or human cell lines or Caenorhabditis elegans. Cubebin can be used for the research of diabetic nephropathy, melanoma, colon adenocarcinoma, neuroangiostrongyliasis, Alzheimer’s disease (AD) and depression .
TLR7 agonist 1 is a selective TLR7 agonist with an LEC value of 90 nM. TLR7 agonist 1 activates downstream immune regulation and shows no activity against TLR8. TLR7 agonist 1 induces endogenous IFN-α production in mice .
Sasanlimab is a humanized IgG4 isotype anti-PD-1 antibody. Sasanlimab blocks PD-1 interaction with PD-L1/PD-L2, reverses PD-1-mediated inhibitory T-cell signaling, augments T-cell proliferation and cytokine production. Sasanlimab inhibits colon adenocarcinoma tumor growth, and accelerates graft-versus-host disease incidence via enhanced T-cell activity. Sasanlimab can be used for the research of cancer, such as bladder cancer and colon adenocarcinoma .
AL002 is a humanized monoclonal IgG1 antibody and a blood-brain barrier-permeable TREM2 modulator. AL002 binds to TREM2 on the surface of microglia, promotes TREM2 clustering and the formation of the TREM2-DAP12 complex, activates the TREM2 signaling pathway and PI3K cascade, and induces TREM2 internalization and degradation. AL002 is applicable to research related to Alzheimer's disease .
GSK1995057 is a human monoclonal antibody (mAb) targeting TNFRSF1A. GSK1995057 selectively binds to TNFR1, blocks the binding of TNF-α and LT-α, and does not interfere with TNFR2 signaling. GSK1995057 inhibits the activation of NF-κB, JNK and MAPK pathways, alleviates apoptosis (apoptosis) and inflammatory responses (inhibiting IL-1β, IL-6, IL-10, TNF-α), and prevents viability loss of human nucleus pulposus cells. GSK1995057 inhibits the expression of cytokines and neutrophil adhesion molecules in human pulmonary microvascular endothelial cell monolayers, and reduces inflammatory responses and lung injury symptoms in non-human primates. GSK1995057 forms complexes with HAVH autoantibodies, thereby activating TNFR1 and triggering the release of cytokines and IL-8 in human cells. GSK1995057 can be used in research related to intervertebral disc degeneration and acute lung injury .
NMB04 is a recombinant anti-Human CD257 (BAFF) (BLyS) antibody. NMB04 binds with specificity and high affinity to soluble and membrane-bound Blys, and blocks Blys binding to receptors TACI, BCMA, and BR-3. NMB04 can be used for the research of autoimmune diseases .
GATT-44 is a blood-brain barrier-permeable, selective GABA transporter 1 (GAT-1) ligand with an IC50 of 126 nM. GATT-44 shows selectivity for GAT-2, GAT-3 and BGT-1 subtypes, and undergoes copper-mediated 18F-radiofluorination. The radiolabeled GATT-44 ([ 18F]GATT-44) exhibits brain uptake, metabolic stability and high GAT-1 binding specificity in non-human primates. GATT-44 is applicable for research on neurodegenerative and neuropsychiatric diseases .
AZD3783 is an orally active, blood-brain barrier-penetrant 5-HT1B receptor antagonist. AZD3783 reverses agonist-induced hypothermia, inhibits separation-induced vocalizations in guinea pig pups, and acts as a moderately permeable glycoprotein substrate with moderate clearance. AZD3783 inhibits hERG channel activity. AZD3783 is applicable for research on depression, anxiety disorders, and other psychiatric diseases associated with serotonergic neurotransmission .
15(R)-17-phenyl trinor Prostaglandin F2α isopropyl ester (15(R)-17-phenyl trinor PGF2α isopropyl ester) is the latanoprost-related isomer containing both a double bond at 13,14 and an inverted (β) hydroxyl group at C-15. Similar to 15(S)-latanoprost, 15(R)-17-phenyl trinor PGF2α isopropyl ester is a potential impurity in most commercial preparations of the latanoprost bulk drug product. The IC50 values for the free acid forms of 15(S)-17-phenyl trinor PGF2α and 15(R)-17-phenyl trinor PGF2α were determined to be 0.71 nM and 30 nM, respectively, in a FP receptor binding assay using the cat iris sphincter muscle.1 A 3 μg dose of 15(R)-17-phenyl trinor PGF2α caused a 1.9 mmHg reduction of IOP in normotensive cynomolgus monkeys.
17-Phenyl trinor PGF2α isopropyl ester is a FP receptor agonist and intraocular pressure-lowering agent. 17-Phenyl trinor PGF2α isopropyl ester induces iris sphincter contraction, reduces intraocular pressure and pupil diameter, causes no ocular irritation, and only leads to mild conjunctival hyperemia. 17-Phenyl trinor PGF2α isopropyl ester is applicable to relevant research on glaucoma .
AVID100 Antibody (MAB100) is a monoclonal antibody inhibitor targeting EGFR, which can be used to synthesize a novel antibody-drug conjugate (ADC) molecule AVID100. AVID100 Antibody is applicable to relevant research on breast cancer, head and neck cancer, and lung cancer .
Zelebrudomide (NX-2127) (Compound 28) is an orally active PROTAC deggrader, targeting to Bruton’s Tyrosine Kinase (Btk). Zelebrudomide inhibits proliferation of BTK C481S mutant TMD8 cells, more effectively than Ibrutinib (HY-10997). Zelebrudomide catalyzes the degradation of Ikaros (IKZF1) and Aiolos (IKZF3) with of 25 nM and 54 nM, respectively. Zelebrudomide stimulates T cell activation and increases IL-2 production in primary human T Cells . (Pink: BTK ligand 10 (HY-168302); Black: (R)-4-(1-(Pyrrolidin-3-ylmethyl)piperidin-4-yl)aniline (HY-168348); Blue: Thalidomide 5-fluoride (HY-W087383)
SOT102 Antibody is an IgG1 monoclonal antibody targeting CLDN18.2. SOT102 Antibody binds selectively to CLDN18.2, and promotes internalization. SOT102 Antibody can be used for the research of cancer [2].
APG808 is an anti-human IL-4Rα monoclonal antibody. APG808 binds to IL-4Rα, prevents IL-13Rα1/IL-4Rα heterodimer formation, and disrupts IL-13 and IL-4 mediated signaling. APG808 ablates Fc and complement effector functions. APG808 can be used for the research of chronic obstructive pulmonary disease, asthma, atopic dermatitis .
MC-cBu-Cit-seco-CBI dimer (Compound 10) is a conjugate of an ADC drug toxin molecule and a linker, which consists of a DNA alkylating agent connected to a reactive maleimide via a protease-cleavable peptidomimetic linker .
RFB4 is an anti-CD22 monoclonal antibody. RFB4 can be fused with Pseudomonas aeruginosa exotoxin (PE38) via disulfide bonds to construct recombinant immunotoxins, such as RFB4 (dsFv)-PE38. RFB4 is applicable to the research of cancers including lymphoma .
Vixticibart (REGN-5381) is a fully human IgG4 monoclonal antibody and NPR1 agonist that targets NPR1. Vixticibart stabilizes the receptor in an activated conformation by binding to the N-terminal domain of NPR1, and enhances the activity of endogenous ligands ANP and BNP without blocking ligand binding when these ligands are present. Vixticibart exerts vasodilatory and hypotensive effects by inducing cGMP production, preferentially dilating venous vessels to reduce systolic and venous pressure, but does not induce diuresis and may trigger a compensatory increase in heart rate. Vixticibart produces a synergistic hypotensive effect when combined with angiotensin-converting enzyme inhibitors or angiotensin receptor blockers, and is currently mainly used in research related to heart failure and hypertension .
Sepetaprost (ONO-9054) is a dual agonist of the prostaglandin E3 receptor and prostaglandin F receptor. Sepetaprost reduces intraocular pressure in animal models. Sepetaprost is applicable for research on ocular hypertension and open-angle glaucoma .
Eicosatetraynoic acid (ETYA) is a non-metabolizable analog of Arachidonic acid (HY-109590) and also an inhibitor of the lipoxygenase (LOX)/cyclooxygenase (COX) pathway (ID50= 8 μM and 4 μM). Eicosatetraynoic acid acts as a suicide substrate to inhibit the production of inflammatory mediators such as leukotrienes and prostaglandins. Eicosatetraynoic acid acts directly on cell membranes and membrane proteins to exert a wide range of effects, including blocking potassium channels, increasing cell membrane fluidity, elevating intracellular calcium levels, inhibiting DNA synthesis in tumor cells, inducing differentiation of certain cells, and specifically inhibiting the assembly and replication of orthopoxviruses. Eicosatetraynoic acid alleviates acute lung injury induced by chemicals such as phosgene .
Olpasiran (AMG 890, ARC-LPA) sodium is an N-acetyl galactosamine (GalNAc)-conjugated, hepatocyte-targeted siRNA. Olpasiran sodium directly inhibits LPA messenger RNA translation in hepatocytes and potently reduce Lp(a) concentration. Olpasiran sodium can be used for the research of cardiovascular disease, such as atherosclerosis .
TLC-2716 is an orally available, gut- and liver-restricted inhibitor against LXRα and LXRβ, with EC50 values of 7 nM and 15 nM, respectively. TLC-2716 represses LXRα/β transcriptional activity, downregulates genes involved in lipogenesis, lipid absorption and lipoprotein metabolism, and preserves peripheral reverse cholesterol transport. TLC-2716 reduces lipid accumulation, suppresses inflammation and fibrotic gene expression, enhances triglyceride-rich lipoprotein clearance, and improves glucose homeostasis and insulin sensitivity. TLC-2716 lowers serum and hepatic triglycerides, plasma cholesterol and other atherogenic lipid profiles in experimental models and humanized liver mice. TLC-2716 can be used for the research of dyslipidemia and related cardiometabolic disorders .
GLP-1R-agonist-43 (Compound A) is an orally active GLP-1R agonist with an EC50 of 2.68 nM. GLP-1R-agonist-43 can be used in the research of non-insulin-dependent diabetes mellitus (type 2 diabetes) and obesity .
PF-06650808 Antibody (Anti-NOTCH3 mAb hu28) is an IgG1-kappa Notch3-targeting antibody. PF-06650808 Antibody is the antibody component of the antibody-drug conjugate (ADC) PF-06650808. PF-06650808 Antibody can be used for the research of advanced breast cancer, advanced solid tumors .
Zomepirac sodium salt (Standard) is the analytical standard of Zomepirac sodium salt (HY-B0890). This product is intended for research and analytical applications. Zomepirac sodium salt (McN-2783-21-98) is an orally active prostaglandin synthetase inhibitor. Zomepirac sodium salt blocks prostaglandin synthesis and inhibits Collagen (HY-P72147)- or Epinephrine (HY-B0447)-induced platelet aggregation. Zomepirac sodium salt can be used for the research of postoperative pain and osteoarthritis .
Zomepirac (McN-2783-21-98 free acid) is an orally active prostaglandin synthetase inhibitor. Zomepirac blocks prostaglandin synthesis and inhibits Collagen (HY-P72147)- or Epinephrine (HY-B0447)-induced platelet aggregation. Zomepirac can be used for the research of postoperative pain and osteoarthritis .
DB-1310 Antibody is a monoclonal antibody inhibitor targeting HER3. DB-1310 Antibody can be used to synthesize the antibody-drug conjugate (ADC) DB-1310. DB-1310 Antibody is applicable to research related to HER3-positive solid tumors, non-small cell lung cancer, breast cancer, colon cancer and prostate cancer .
Zomepirac sodium salt (McN-2783-21-98) is an orally active prostaglandin synthetase inhibitor. Zomepirac sodium salt blocks prostaglandin synthesis and inhibits Collagen (HY-P72147)- or Epinephrine (HY-B0447)-induced platelet aggregation. Zomepirac sodium salt can be used for the research of postoperative pain and osteoarthritis .
Nipamovir is an anti-HIV prodrug. Nipamovir is cleaved in vivo by glutathione and other active thiols. Nipamovir inhibits the replication of HIV-1RF and HIV-192HT599 in cells, with EC50 values of 3.64 μM and 3.23 μM, respectively. Nipamovir can be used in studies related to HIV infection .
Denecimig (Mim8) is a factor VIII-mimetic bispecific antibody with micromolar human binding affinity for Factor X and Factor IXa. Denecimig binds Factor X and Factor IXa, localizes both to the phospholipid surface, enhances the Factor IXa-mediated activation of Factor X to Factor Xa, and stimulates the proteolytic activity of Factor IXa via its monovalent anti-Factor IXa arm. Denecimig is applicable to research related to hemophilia A.
Misitatug blivedotin (RC88) is an antibody-drug conjugate (ADC) targeting mesothelin (MSLN). Misitatug blivedotin binds to mesothelin and exhibits dose‐dependent antitumor activity. Misitatug blivedotin can be used for the research of ovarian cancer, non-squamous non-small-cell lung carcinoma, cervical cancer .
seco-CBI dimer is a DNA alkylating agent and a prodrug of Duocarmycin, which can serve as a payload for synthesizing antibody-drug conjugates (ADCs). seco-CBI dimer binds to the minor groove of A-T-rich regions in DNA, alkylates the N3 position of adenine residues, and induces DNA strand breaks. seco-CBI dimer can be used in the research of non-Hodgkin's lymphoma .
LR004 is an EGFR monoclonal antibody, with a Kd of 2.80 × 10 -9 M against human EGFR. LR004 shows extremely weak inhibitory effect on the viability of EGFR-positive tumor cells in vitro, but inhibits the growth of EGFR-positive tumor xenografts as a single agent. LR004 is applicable to research related to advanced colorectal cancer, solid tumors, esophageal squamous cell carcinoma, epidermoid carcinoma, colon cancer and breast cancer .
Custirsen (OGX-011) is an antisense oligonucleotide that targets clusterin mRNA. Custirsen induces apoptosis by activating Bax, triggering mitochondrial translocation and cytochrome c release. Custirsen acts as a chemosensitizer, radiosensitizer and hormone sensitizer. Custirsen can be used in research related to prostate cancer, non-small cell lung cancer and metastatic breast cancer .
SAR-443809 is a selective alternative complement system inhibitor and monoclonal antibody targeting complement factor Bb. SAR-443809 blocks the cleavage of C3 and factor B by selectively binding to the activated form of factor Bb, with a KD of 7.3 nM for human factor Bb. SAR-443809 inhibits the amplification loop of the alternative complement pathway and C3 activation, reduces C3b deposition, and blocks the activation of pathways associated with intravascular and extravascular hemolysis. SAR-443809 can be used for the research of hematological and renal disorders mediated by abnormal alternative complement pathway .
Cizutamig (CND-106) is a bispecific T-cell engager targeting BCMA and CD3. Cizutamig exhibits immunostimulatory and anti-tumor activities. Cizutamig can be used in research related to relapsed or refractory multiple myeloma and systemic lupus erythematosus .
JNJ-55920839 (CNTO-6358) is a fully human immunoglobulin G1κ monoclonal antibody and a selective Interferonα/ω neutralizer, with a Kd value of 0.9-10.7 pM against hIFNα and a Kd of 1.44 pM against IFNω. JNJ-55920839 can be used in research related to systemic lupus erythematosus .
Z-Val-Ala-OH is a dipeptide derivative of valine and alanine. Z-Val-Ala-OH undergoes cleavage by cathepsin B and other lysosomal proteases to enable payload release following lysosomal internalization.Z-Val-Ala-OH can be used for the research of antibody-drug conjugate (ADC) development[1] .
Itanistomig (LB-101) is a tetravalent bispecific antibody targeting PD-L1 and CD47. Itanistomig blocks PD-L1 and achieves tumor enrichment through binding to PD-L1, and also exerts conditional CD47 blocking activity via cleavage of the hinge linker in the PD-L1-positive tumor microenvironment. Itanistomig induces antibody-dependent cellular phagocytosis in human CD14 + cells and drives tumor regression. Itanistomig can be used in research related to solid tumors .
FXIa/Plasma kallikrein-IN-1 is an inhibitor of coagulation factor XIa (FXIa) and plasma kallikrein with Ki values of 187.70 nM and 151.6 nM, respectively. FXIa/Plasma kallikrein-IN-1 can be used in the research of thromboembolic diseases .
Veligrotug (AVE1642) is a selective, fully human IGF-1R antagonist antibody with a Kd value of 0.55 nM for hIGF-1R. Veligrotug blocks the phosphorylation of downstream AKT. Veligrotug is applicable to research related to thyroid eye disease .
Bax activator-2 (compound 27c) is a pro-apoptotic agent targeting BAX, with an IC50 of 0.30 μmol/L against human BAX. Bax activator-2 binds to the trigger site of BAX and induces its conformational change. Bax activator-2 induces mitochondrial depolarization, cytochrome c release, caspase-3/9 cleavage and PARP cleavage, thereby initiating apoptosis. Bax activator-2 exhibits cytotoxicity against various cancer cell lines, shows reduced cytotoxicity in BAX-knockout A549 cells, and has low cytotoxicity against non-cancerous cell lines. Bax activator-2 can be used in studies related to acute myeloid leukemia and solid tumors .
Zubotamig (Gen1047) is an CD3E/VTCN1-targeting Ig(G1 -κ_G1 -λ2) type chimeric human antibody. The recommed isotype control is Human IgG1 kappa, Isotype Control (HY-P99001). Zubotamig induces T-cell mediated cytotoxicity of B7H4-positive tumor cells, triggers T-cell activation, and induces cytokine release from T cells in the presence of B7H4-expressing tumor cells. Zubotamig demonstrates antitumor activity in mouse patient-derived xenograft (PDX) models. Zubotamig can be used for the research of solid cancers (including breast, ovarian and lung cancer) .
Mal-Val-Ala-PAB-N(SO2Me)-Exatecan (Compound LE14) is a conjugate of an ADC toxin Exatecan (HY-13631) and a linker Mal-Val-Ala-PAB-N(SO2Me). Mal-Val-Ala-PAB-N(SO2Me)-Exatecan can be used for synthesis of ADC FZ-AD005. FZ-AD005 is a delta-like ligand 3 (DLL3, KD=58.3 pM) targeting ADC, that exhibits antitumor efficacy against SCLC cancer .
Emirodatamab (AMG-427) is a bispecific T-cell engager (BiTE). Emirodatamab simultaneously binds FLT3 on the surface of acute myeloid leukemia (AML) cells and CD3 on the surface of T cells, thereby precisely recruiting immune effector cells to tumor sites. Emirodatamab potently induces T cell activation, secretion of proinflammatory cytokines (such as IFNγ, TNFα), and specific cytotoxicity, effectively lysing FLT3-positive tumor cells and inhibiting their growth. Emirodatamab not only significantly prolongs survival in mouse xenograft models and eliminates diseased cells in primates, but also exhibits a synergistic enhancement effect when combined with PD-1 blockade therapy. Emirodatamab is used in studies of acute myeloid leukemia, especially relapsed or refractory cases .
SHR-2010 is a fully humanized monoclonal antibody targeting MASP-2. SHR-2010 selectively inhibits lectin pathway activation without affecting classical or alternative complement pathways. SHR-2010 can be used for the research of IgA nephropathy .
SX-576 is a CXCR1 and CXCR2 antagonist with IC50 values of 31 nM and 21 nM, respectively. SX-576 inhibits neutrophil infiltration in a rat model of pulmonary inflammation. SX-576 can be used in studies related to pulmonary inflammation .
Ifinatamab deruxtecan (DS-7300a) is a B7-H3-targeting Antibody-drug conjugate (ADC), which is composed of a humanized anti-B7-H3 monoclonal antibody, an enzymatically cleavable peptide-based linker, and Exatecan derivative (DXd) (HY-13631D). Ifinatamab deruxtecan is a DNA Topoisomerase I inhibitor. Ifinatamab deruxtecan induces Apoptosis. DS-7300a exerts potent antitumor activities against B7-H3-expressing tumors. against rhabdomyosarcoma, endometrial adenocarcinoma and lung adenocarcinoma. Ifinatamab deruxtecan does not exert direct immunomodulatory effects
SCH 351591 is a highly selective, orally active PDE4 inhibitor, with IC50 values of 58 nM and 153 nM in humans and rats, respectively. SCH 351591 effectively inhibits pathological processes such as cytokine production, eosinophilia, airway hyperresponsiveness and bronchospasm. SCH 351591 also induces microvascular injury, activates mast cells and endothelial cells, and causes increases in serum histamine and various inflammatory factors, leading to early vascular damage. SCH 351591 has been widely used in studies related to asthma, chronic obstructive pulmonary disease and drug-induced vascular injury .
Anzurstobart is a CD47/SIRPα inhibitor with human SIRPα Kd of 0.0541 nM and human SIRPα IC50 of 100 nM.Anzurstobart binds SIRPα at a CD47-overlapping site, blocks CD47-SIRPα interactions, inhibits CD47-SIRPα axis signaling, and binds across 6 prevalent human SIRPα haplotypes.Anzurstobart binds SIRPγ and inhibits CD47-SIRPγ interactions.Anzurstobart can be used for the research of non-Hodgkin's lymphoma, colorectal cancer, squamous cell carcinoma of the head and neck, diffuse large B-cell lymphoma, and advanced solid and hematologic malignancies .
Surovatamig (AZD0486; TNB-486) is a fully human anti-CD19/CD3 IgG4 bispecific antibody. Surovatamig triggers T cell activation, releases cytotoxic granules, and induces T cell-dependent cellular cytotoxicity and tumor cell lysis. Surovatamig can reduces release of pro-inflammatory cytokines including IL-2, IFNγ, TNF. Surovatamig can be used for the research of cancer, such as B cell non-Hodgkin lymphoma .
BR103354 is an orally active, selective fibroblast activation protein (FAP) inhibitor with an IC50 value of 14 nM against hFAP. BR103354 restores the levels of phosphorylated ERK and Glut1 that are reduced by co-treatment with hFGF21 and FAP, decreases non-fasting blood glucose concentrations, improves glucose tolerance, and reduces hepatic triglyceride content. BR103354 ameliorates hepatic steatosis and hepatic fibrosis. BR103354 can be used in the research of type 2 diabetes and non-alcoholic steatohepatitis .
REGN-7257 is a humanized monoclonal antibody targeting IL2RG. REGN-7257 blocks the signal transduction induced by common gamma chain (γc) cytokines via the IL2RG chain of the γc cytokine receptor complex. REGN-7257 is applicable for research on immune-mediated diseases and T cell-mediated diseases . Its corresponding isotype control is Human IgG4 kappa, Isotype Control (HY-P99003).
Etedesiran is a component of the AOC drug Delpacibart etedesiran (HY-177565), formed by the reaction of an siRNA that induces cleavage of mRNA encoding myotonic dystrophy protein kinase (MTPK or DMPK) with SMCC linker (HY-42360). Etedesiran carries a maleimide group at its terminus, which can react with cysteine or lysine and is used for the synthesis of AOC drugs. Etedesiran is applicable to research related to myotonic dystrophy type 1 .
PF-06817024 is a high affinity, humanized antibody that binds IL-33. PF-06817024 binds to IL-33, prevents IL-33 from binding to receptor ST2, and inhibits downstream type 2 inflammatory responses. PF-06817024 can be used for the research of allergic diseases .
Sacituzumab tirumotecan is an antibody-drug conjugate and TROP2-directed, topoisomerase I inhibitor payload-delivering agent, with a TROP2EC50 of 2.787 ng/ml, TROP2Ka of 0.3083 nM, and topoisomerase I IC50 of 0.7 μmol/L. Sacituzumab tirumotecan can be used for the research of metastatic triple-negative breast cancer, and metastatic non-small cell lung cancer .
SHR-1802 is a humanized anti-LAG-3 monoclonal antibody.SHR-1802 specifically binds to LAG-3 and inhibits its binding to major histocompatibility complex class II (MHC-II), fibrinogen-like protein 1 (FGL1), galectin-3, and liver sinusoidal endothelial cell lectin.SHR-1802 can be used for the research of advanced solid tumors .
MDX-1203 (BMS-936561) is an antibody-drug conjugate targeting CD70. MDX-1203 binds to CD70 and mediates the specific delivery of its conjugated cytotoxic payload to tumors. MDX-1203 delivers a DNA alkylating payload into cells. MDX-1203 can be used in research related to advanced clear cell renal cell carcinoma and relapsed/refractory B-cell non-Hodgkin lymphoma .
Ciluprevir (BILN 2061; BILN 2061ZW) is an orally active macrocyclic peptide inhibitor of hepatitis C virus (HCV)NS3 protease, with an IC50 of 3 nM. Ciluprevir has Kᵢ values of 0.66 nM and 0.30 nM against genotypes 1b and 1a, respectively. Ciluprevir inhibits HCV RNA replication with an EC50 of 1.2 nM, and its EC50 values against genotypes 1b and 1a are 3 nM and 4 nM, respectively. Ciluprevir shows no significant inhibition against human leukocyte elastase and hepatic cathepsin B. Ciluprevir can be used for genotype 1 HCV infection .
Amtabafusp alfa (GS-8588) is an envelope-targeting bispecific T-cell engager for HIV treatment. Amtabafusp alfa redirects effector T cells by binding to CD3 via a humanized anti-CD3 Fab domain and to HIV envelope proteins via an engineered CD4 domain 1 variant. Amtabafusp alfa exhibits potent, broad-spectrum activity against a variety of HIV isolates and specifically kills HIV-infected cells. Amtabafusp alfa can be used for research on HIV infection .
Inotersen (GSK-2998728; ISIS-420915) is a 2'-O-methoxyethyl-modified antisense oligonucleotide and transthyretin (TTR) inhibitor with low genotoxicity. Inotersen triggers RNase H1-mediated degradation by binding to TTR mRNA, thereby effectively reducing the production of both mutant and wild-type transthyretin in the liver. Inotersen significantly reduces amyloid fiber deposition, yet specific toxicities such as inflammation or tumors are observed at high doses in some animal models. Inotersen is used in studies of hereditary transthyretin amyloidosis and the associated polyneuropathy and cardiomyopathy .
Anti-Human/Mouse LY6E Antibody (9B12) is a high-affinity, multi-target antibody that binds specifically to LY6E. Anti-Human/Mouse LY6E Antibody (9B12) binds specifically to cell-surface LY6E and enters lysosomes via lipid raft-dependent endocytosis, thereby effectively inhibiting the growth of various LY6E-expressing solid tumors (such as breast cancer and lung cancer) in both in vitro and in vivo models. Anti-Human/Mouse LY6E Antibody (9B12) exerts a dual mechanism of action: on one hand, it blocks the interaction between PILRα and CD8α, specifically reduces the survival rate of peripheral CD8 + T cells and induces their activation, breaking the state of cellular quiescence; on the other hand, it recognizes and immunoprecipitates IDE under both non-denaturing and denaturing conditions, which is applicable to studies on the subcellular localization and protein interactions of IDE. The regulatory effect of Anti-Human/Mouse LY6E Antibody (9B12) on CD8 + T cells strictly depends on the presence of PILRα, and it does not affect CD4 + T cells or T cell development in the thymus, exhibiting high specificity .
AG-024104 is a CDK inhibitor with Ki values of 2.3 nM (CDK1/cyclinB), 1.8 nM (CDK2/cyclinA), and 0.67 nM (CDK4/cyclinD). AG-024104 functionally inhibits kinase activity of CDK1/cyclinB, CDK2/cyclinA, and CDK4/cyclinD. AG-024104 serves as a negative control for peripheral leukocyte toxicity studies in preclinical development .
CHDI-340246 is an orally active kynurenine monooxygenase (KMO) inhibitor. CHDI-340246 blocks KMO activity, alters the metabolic flux of the kynurenine pathway, inhibits the production of 3-hydroxykynurenine and quinolinic acid, elevates the levels of kynurenine and kynurenic acid, and restores electrophysiological abnormalities in transgenic mouse models of Huntington's disease. CHDI-340246 can be used in studies related to Huntington's disease .
Ancitabine hydrochloride is a cytarabine derivative that inhibits viral replication. Ancitabine hydrochloride blocks vaccinia virus DNA replication, the progression of viral protein synthesis from early to late stages, and one-step growth of vaccinia virus. Ancitabine hydrochloride is applicable to research related to vaccinia virus infection, leukemia, human cytomegalovirus infection and colorectal cancer .
NT-0527 is a selective, orally active, and brain-permeable NLRP3 inflammasome inhibitor. NT-0527 can specifically block the formation of the NLRP3 inflammasome, resulting in the reduction in the maturation and release of IL-1β, exhibit inhibition on CYP2C19. NT-0527 displays anti-inflammatory activity in the mouse LPS (HY-D1056) /ATP (HY-B2176)-induced peritonitis model. NT-0527 can be used for the research of neuroinflammatory disorders (Parkinson's disease, Alzheimer's disease, amyotrophic lateral sclerosis) and peripheral inflammatory disorders (type II diabetes, atherosclerosis, gout, etc.) associated with NLRP3 inflammasome .
TNX-1500 is a crystallizable fragment-modified anti-CD154 antibody. TNX-1500 contains the hu5c8 fragment antigen-binding (Fab) domain from Ruplizumab (HY-P99315) and an IgG4 Fc region engineered to reduce FcγRIIa binding. TNX-1500 has significantly weaker binding affinity to FcγRI, FcγRIIaH, FcγRIIbF, FcγRIIIaF, and FcγRIIIaV compared to hu5c8 (Kdvalues: 8.7 nM, 7100 nM, 4900 nM, 8000 nM, 6000 nM respectively). TNX-1500 prolongs nonhuman primate renal allograft survival, prolongs nonhuman primate cardiac allograft survival. TNX-1500 can be used for the research of allograft rejection [1][2].
Sacituzumab tirumotecan is an antibody-drug conjugate and TROP2-directed, topoisomerase I inhibitor payload-delivering agent, with a TROP2EC50 of 2.787 ng/ml, TROP2Ka of 0.3083 nM, and topoisomerase I IC50 of 0.7 μmol/L. Sacituzumab tirumotecan can be used for the research of metastatic triple-negative breast cancer, and metastatic non-small cell lung cancer .
Ifinatamab deruxtecan (DS-7300a) is a B7-H3-targeting Antibody-drug conjugate (ADC), which is composed of a humanized anti-B7-H3 monoclonal antibody, an enzymatically cleavable peptide-based linker, and Exatecan derivative (DXd) (HY-13631D). Ifinatamab deruxtecan is a DNA Topoisomerase I inhibitor. Ifinatamab deruxtecan induces Apoptosis. DS-7300a exerts potent antitumor activities against B7-H3-expressing tumors. against rhabdomyosarcoma, endometrial adenocarcinoma and lung adenocarcinoma. Ifinatamab deruxtecan does not exert direct immunomodulatory effects
Maridebart cafraglutide (AMG 133) is a long-acting peptide-antibody conjugate that combines GLP-1 receptor agonist with glucose-dependent insulinotropic polypeptide (GIP) receptor antagonism. Maridebart cafraglutide shows antagonist activity against human, cynomolgus monkey and rat GIPR with IC50 values of 46.4 nM, 26.5 nM, 822.3 nM, respectively. Maridebart cafraglutide shows agonist activity against human, cynomolgus monkey, rat and mouse GLP-1R with EC50 values of 24.4 pM, 5.7 pM, 2.4 pM and 123 pM, respectively. Maridebart cafraglutide can be used for the study of obesity and type 2 diabetes .
FZ-AD005 is a DLL3-targeting antibody-drug conjugate (ADC) with high selectivity, composed of the anti-DLL3 antibody FZ-A038 (HY-P990896), a dipeptide linker (Val-Ala), and DXd (HY-13631D). The Kd value of FZ-AD005 for human DLL3 ranges from 13.29 to 58.3 pmol/L. After binding to DLL3 on the cell surface, FZ-AD005 mediates endocytosis, and the payload DXd is released via cleavage by lysosomal cathepsins. DXd inhibits topoisomerase TopI to induce double-strand DNA breaks, cell cycle arrest and apoptosis, and FZ-AD005 exhibits bystander killing activity against adjacent DLL3-negative cells. FZ-AD005 shows stable circulation in vivo, has good tolerance and acceptable pharmacokinetic profiles in rats and cynomolgus monkeys, and effectively inhibits the growth of DLL3-expressing tumor cells. FZ-AD005 serves as a promising candidate molecule for research on small cell lung cancer and human neuroendocrine prostate cancer .
ABBV-154 is an anti-TNF antibody-drug conjugate (ADC). ABBV-154 is composed of the humanized antibody Adalimumab (HY-P9908) conjugated with a glucocorticoid receptor modulator (HY-137883). ABBV-154 can be used in studies of rheumatoid arthritis, Crohn's disease and polymyalgia rheumatica .
Cholesteryl oleate is an ester compound formed from Cholesterol (HY-N0322) and Oleic acid (HY-N1446), which is involved in lipid transport, storage and cell membrane formation in living organisms. Cholesteryl oleate may serve as a potential biomarker for prostate cancer. Cholesteryl oleate can also prepare cationic solid lipid nanoparticles (SLNs) for efficient gene silencing .
Cynomolgus Monkey serum albumin is a plasma protein derived from cynomolgus monkey. Serum albumin is a multifunctional protein with extraordinary ligand binding capacity, making it a transporter molecule for a diverse range of metabolites, drugs, nutrients, metals and other molecules.
Glyceryl trinonanoate is a triacylglycerol containing nonanoic acid at the sn-1, sn-2 and sn-3 positions. It has been found in Schizochytrium biomass. 1 1,2,3-Trinonanoyl-rac-glycerol increases blood levels of the ketone body D-(-)-3-hydroxybutyrate in neonatal rhesus monkeys. 2|1. Mioso, R., Toledo Marante, FJ, González, JE, et al. Schizochytrium sp. metabolite analysis. Oleaginous microbial sources of biodiesel by GC-MS. braz. J. Microbiology. 45(2), 403-409 (2014).|2. Tetrick, MA, Greer, FR and Benevenga, NJ Blood D- ( )-3-Hydroxybutyric acid concentration. Compare. medicine. 60(6), 486-490 (2010).
Cynomolgus Monkey haptoglobin is a hemoglobin-binding protein derived from cynomolgus monkeys. Cynomolgus Monkey haptoglobin is generally assumed to be analogous to human serum haptoglobin (Hp) .
Cynomolgus Monkey transferrin is a cynomolgus monkey-derived protein. Transferrin is the transport of iron in the bloodstream. Transferrin can also act as a growth factor .
Type II Collagen, T Cell Grade, from Monkey is a T-cell dependent antigen with unique immunological features. Type II Collagen, T Cell Chick, from Monkey can be used as a stimulating antigen for T-cells in in vitro culture systems .
AMG133 peptide payload TFA is a GLP-1 analog agonist peptide. AMG133 peptide payload TFA potently activates GLP-1R and exhibits weight loss and metabolic improvement activities. AMG133 peptide payload TFA can be used for the synthesis of AMG 133 (HY-164535) .
AMG133 peptide payload is a GLP-1 analog agonist peptide. AMG133 peptide potently activates GLP-1R, and exhibits weight loss and metabolic improvement activities. AMG133 peptide payload can be used for the synthesis of AMG 133 (HY-164535) .
SAR441255 is a potent unimolecular peptide GLP-1/GIP/GCG receptor triagonist. SAR441255 displays high potency with balanced activation of all three target receptors.?SAR441255 shows positive acute glucoregulatory effectss in diabetic obese monkeys .
Bofanglutide (GZR18) is an analog of glucagon-like peptide-1 (GLP-1), which exhibits agonistic activity for GLP-1 receptor, with an EC50 of 0.677 nM. GZR18 ameliorates type 2 diabetes .
Z-Val-Ala-OH is a dipeptide derivative of valine and alanine. Z-Val-Ala-OH undergoes cleavage by cathepsin B and other lysosomal proteases to enable payload release following lysosomal internalization.Z-Val-Ala-OH can be used for the research of antibody-drug conjugate (ADC) development[1] .
Peptide M is a synthetic amino acid (18 amino acids in length which correspond to the amino acid positions 303-322 of bovine S-antigen: DTNLASSTIIKEGIDKTV), is capable of inducing experimental autoimmune uveitis in monkeys and Hartley guinea pigs as well as Lewis rats .
β-MSH (monkey) is a polypeptide that can be found by peptide screening. Peptide screening is a research tool that pools active peptides primarily by immunoassay. Peptide screening can be used for protein interaction, functional analysis, epitope screening, especially in the field of agent research and development .
SAR441255 TFA is a potent unimolecular peptide GLP-1/GIP/GCG receptor triagonist. SAR441255 TFA displays high potency with balanced activation of all three target receptors.?SAR441255 TFA shows positive acute glucoregulatory effectss in diabetic obese monkeys .
SHR-2042 is a selective agonist of the GLP-1 receptor.SHR-2042 improves glycemic control by activating the GLP-1 receptor, enhancing insulin secretion and inhibiting glucagon secretion. SHR-2042 combined with sodium N-(8-[2-hydroxybenzoyl] amino) caprylate (SNAC) promotes monomerization through the formation of micelles and improves oral absorption efficiency .
RL-37 is an alpha-helical antimicrobial peptide. RL-37 can be isolated for rhesus monkey bone marrow. RL-37 rapidly permeabilizes the membranes of Escherichia coli ML-35p and lysed liposomes. RL-37 has effective antibacterial activity against staphylococci, such as wild-type and Methicillin (HY-121544)-resistant S. aureus strains and S. epidermidis ATCC 49741. RL-37 can be used for human skin infections research .
CBLB 612 is an anti-radiation agent. CBLB 612 can be used in the propagation of mouse and monkey moderate stimulation hematopoietic stem cell (HSC), and lure that they are passed to peripheral blood from bone marrow into. CBLB 612 is an important auxiliary agent for cancer .
MOG (92–106), mouse, rat is a biological active peptide. (This is amino acids 92 to 106 fragment of the myelin oligodendrocyte glycoprotein (MOG) from mouse/rat. Mice with MOG (92–106)-induced experimental autoimmune encephalomyelitis develop extensive B cell reactivity against secondary myelin antigens. Despite the fact that this MOG peptide induces only weak T cell responses, MOG-induced autoimmunity is very severe. This peptide is encephalitogenic in SJL mice, DA rats, and rhesus monkeys.)
Ponsegromab is a Growth differentiation factor 15 (GDF15) inhibitor with human, cynomolgus monkey, and mouse target IC50 values of 0.123 nM, 0.053 nM, and 0.102 nM, respectively . Ponsegromab acts as a chemosensitizer, increases intracellular reactive oxygen species, reduces glutathione levels . Ponsegromab can be used for the research of oxaliplatin-resistant colorectal cancer .
Risankizumab (BI 655066) is a humanised IgG monoclonal antibody, targeting IL-23 p19 subunit (Kd <10 pM) and inhibiting IL-17 production induced by human IL-23 in mouse splenocytes (IC50 = 2 pM). Risankizumab can be used to research immunological and inflammatory disorders such as psoriasis vulgaris, psoriatic arthritis, generalized pustular psoriasis and erythrodermic psoriasis .
Ifinatamab deruxtecan (DS-7300a) is a B7-H3-targeting Antibody-drug conjugate (ADC), which is composed of a humanized anti-B7-H3 monoclonal antibody, an enzymatically cleavable peptide-based linker, and Exatecan derivative (DXd) (HY-13631D). Ifinatamab deruxtecan is a DNA Topoisomerase I inhibitor. Ifinatamab deruxtecan induces Apoptosis. DS-7300a exerts potent antitumor activities against B7-H3-expressing tumors. against rhabdomyosarcoma, endometrial adenocarcinoma and lung adenocarcinoma. Ifinatamab deruxtecan does not exert direct immunomodulatory effects
Guselkumab is a recombinant human IgG1 monoclonal antibody against the IL-23p19 subunit. Guselkumab binds to human and cynomolgus monkey IL-23 with Kd values of 3.3 and 1.9 pmol/L, respectively. Guselkumab inhibits production of cytokines lying downstream of the IL-23 signaling pathway and can be used for psoriatic arthritis research .
Onartuzumab (MetMAb) is a unique, humanized and affinity-matured monovalent (one-armed) monoclonal antibody against the MET receptor. Onartuzumab potently inhibits HGF binding and receptor phosphorylation and signaling. Onartuzumab has antibody-like pharmacokinetics and antitumor activity .
Visugromab (CTL-002) is a GDF-15 neutralizing IgG4 mAb. Visugromab has synergistic anticancer activity with the anti-PD1 antibody Nivolumab (HY-P9903) and can effectively act on PD-1/PD-L1 relapsed/refractory metastatic solid tumors. Recommend Isotype Controls: Human IgG4 (S228P) kappa, Isotype Control (HY-P99003) .
Xaluritamig (AMG-509) is a bispecific T cell engager and cytolytic agent with a Kd of 27.6 nM for human CD3ε. Xaluritamig binds to CD3ε via an anti-CD3 single-chain variable fragment (scFv) domain, and to STEAP1 via a bispecific anti-STEAP1 antigen-binding fragment (Fab) domain, thereby recruiting and activating T cells and forming a bridge between T cells and STEAP1-expressing cancer cells. Xaluritamig induces T cell-mediated redirected cytotoxicity, tumor cell lysis, cytokine release, CD8 + T cell activation and expansion, as well as tumor stasis or regression. Xaluritamig contains an Fc domain with no effector function, which prolongs serum half-life, exhibits only minimal activity against cells with low STEAP1 expression and normal cells, and shows extremely low target-related off-tumor toxicity in cynomolgus monkeys. Xaluritamig is used in STEAP1×CD3 XmAb 2+1 immunotherapy and in research on metastatic castration-resistant prostate cancer and Ewing sarcoma .
Surovatamig (AZD0486; TNB-486) is a fully human anti-CD19/CD3 IgG4 bispecific antibody. Surovatamig triggers T cell activation, releases cytotoxic granules, and induces T cell-dependent cellular cytotoxicity and tumor cell lysis. Surovatamig can reduces release of pro-inflammatory cytokines including IL-2, IFNγ, TNF. Surovatamig can be used for the research of cancer, such as B cell non-Hodgkin lymphoma .
ATR-107 (PF-05230900) is a humanized monoclonal antibody inhibitor that targets the interleukin-21 receptor (IL-21R). The Ka value of ATR-107 is 2-4 nM in cynomolgus monkeys, 16 nM in mice, and 71 nM in rats. ATR-107 can be used in research related to systemic lupus erythematosus and air pouch inflammation .
Mirikizumab (LY3074828) is a humanized IgG4 monoclonal antibody that targets the p19 subunit of interleukin 23 (IL-23). Mirikizumab binds to human and monkeyIL-23 with high affinity, with Kd values of 21 pM and 55 pM, respectively. By inhibiting the binding of IL-23 to IL-23R, Mirikizumab modulates the immune response and holds potential for research in ulcerative colitis and Crohn's disease .
AL002 is a humanized monoclonal IgG1 antibody and a blood-brain barrier-permeable TREM2 modulator. AL002 binds to TREM2 on the surface of microglia, promotes TREM2 clustering and the formation of the TREM2-DAP12 complex, activates the TREM2 signaling pathway and PI3K cascade, and induces TREM2 internalization and degradation. AL002 is applicable to research related to Alzheimer's disease .
Erenumab (AMG-334) is a fully human monoclonal antibody. Erenumab inhibits the calcitonin gene-related peptide (CGRP) receptor. Erenumab prevents the increase in dermal blood flow in cynomolgus monkeys. Erenumab can be used in the research of episodic migraine .
Tanruprubart (ANX005) is a C1q inhibitor and C1q depleter. Tanruprubart is a human antibody expressed in CHO cells, with huIgG1 heavy chains and huκ light chains, and its predicted molecular weight (MW) is 145 kDa. For the isotype control of Tanruprubart, refer to Human IgG1 kappa, Isotype Control (HY-P99001). The IC50 of Tanruprubart is 346 ng/mL for humans and 259 ng/mL for rats; its EC50 is 3.8 ng/mL for humans, 5.2 ng/mL for rats, and 9.9 ng/mL for mice. Tanruprubart is applicable to the research of Guillain-Barré syndrome and Alzheimer's disease .
Stapokibart (CM310) is a humanized monoclonal antibody targeting IL-4Rα (KD values of 0.25 nM, 1.50 nM, and 2.75 nM for human, cynomolgus monkey, and rat IL-4Rα, respectively). Stapokibart effectively blocks the interaction of cytokines IL-4 and IL-13 with their co-receptor subunit IL-4Rα. Stapokibart reduces IL-4 and IL-13 mRNA, inhibits CD23 upregulation, and inhibits IL-4 and IL-13-induced STAT6 activation. Stapokibart improves inflammation (airway inflammation, rhinitis, dermatitis) .
Melredableukin alfa (RG7835) is a bivalent conjugate composed of a human IL-2 mutant (T3A, N88D, C125A) and human IgG1. Melredableukin alfa exhibits enhanced Treg cell selectivity in cynomolgus monkey and humanized mouse models. Melredableukin alfa can be used in research related to ulcerative colitis and autoimmune hepatitis .
Nesfrotamig (YH32367; ABL105) is a bispecific activator targeting HER2 and 4-1BB. The Kd values of Nesfrotamig for human HER2 and human 4-1BB are 0.48 nM and 3.36 nM, respectively. By blocking tumor cell growth signals, activating HER2-dependent local 4-1BB in tumors to maintain T cell survival, and inducing NK cell-mediated antibody-dependent cellular cytotoxicity, Nesfrotamig enhances the cytotoxicity and tumor infiltration ability of immune cells. Nesfrotamig promotes the generation of tumor-specific memory T cells, drives T cell-mediated tumor lysis, exhibits significant anti-tumor efficacy against both HER2-positive and HER2-low-expressing tumors, and shows synergistic activity when combined with anti-PD-1 antibodies. In cynomolgus monkey studies, Nesfrotamig demonstrates good safety and is suitable for research related to HER2-positive and HER2-low-expressing tumors .
Iscalimab (CFZ-533) is a non-depleting IGg1 monoclonal antibody targeting CD40 (KD: 0.3 nM). Iscalimab can be used for research of Graves' hyperthyroidism and autoimmune diseases .
Anti-EphA2 Antibody (1C1) (MEDI-547 antibody) is an anti-EphA2 monoclonal antibody. Anti-EphA2 Antibody (1C1) can induce degradation of EphA2 protein. Anti-EphA2 Antibody (1C1) conjugated with McMMAF (HY-15578) can form an antibody-conjugated drugs, which has potent antitumor activity. Anti-EphA2 Antibody (1C1) can be used for the research of cancer, such as prostate cancer and glioma .
Zigakibart (BION-1301) is an IgG4-kappa, humanized monoclonal antibody against TNFSF13 (tumor necrosis factor (TNF) superfamily member 13, APRIL, CD256). Zigakibart exhibits anti-inflammatory activity .
Cizutamig (CND-106) is a bispecific T-cell engager targeting BCMA and CD3. Cizutamig exhibits immunostimulatory and anti-tumor activities. Cizutamig can be used in research related to relapsed or refractory multiple myeloma and systemic lupus erythematosus .
Emugrobart (GYM-329, RG6237, RG-70240) is a humanized IgG1κ antibody targeting myostatin (Myostatin; GDF8). Emugrobart binds to pro-myostatin and latent myostatin, blocking their cleavage into mature myostatin; it also has a clearance function, which transports bound myostatin for degradation and allows for cyclic reuse. Emugrobart enhances muscle strength in mouse models of muscle atrophy and increases muscle mass in cynomolgus monkeys. Emugrobart can be used in research on spinal muscular atrophy and facioscapulohumeral muscular dystrophy .
Zampilimab (UCB-7858) is a monoclonal antibody against transglutaminase 2 (TG2). Zampilimab inhibits TG2 crosslinking transamidation activity with an IC50 of 0.25 nM and a Kd of <50 pM. Zampilimab improves renal fibrosis .
Semorinemab (RG 6100) is an anti-Tau humanized IgG4 monoclonal antibody, targets the N-terminal portion of the Tau protein (amino acid residues 6-23). Semorinemab binds with human Tau with a Kd value of 3.8 nM. Semorinemab can be used for the research of Alzheimer's Disease .
Margetuximab (MGAH22) is a chimeric anti-HER2 monoclonal antibody optimized Fc domain, with an EC50 value of 39.33 ng/mL. Margetuximab can be used for researching metastatic HER2-positive breast cancer .
Navivumab (CT-P23) is a monoclonal antibody targeting the hemagglutinin (HA) of influenza A virus. Navivumab binds to the HA2 stem fusion domain and the low-variability HA2 region of influenza viruses. Navivumab neutralizes influenza A viruses of subtypes H1, H2, H5, and H9. Navivumab is applicable to research related to influenza and influenza A .
Prezalumab (AMG 557) is a humanized IgG2 monoclonal antibody targeting ICOSL. Prezalumab inhibits T cell activation and related immune responses by binding to ICOSL and blocking the interaction between ICOS and ICOSL. Prezalumab can be used in the research of autoimmune diseases and inflammatory diseases such as systemic lupus erythematosus. Recommend Isotype Controls: Human IgG2 kappa, Isotype Control (HY-P99002) .
GSK1995057 is a human monoclonal antibody (mAb) targeting TNFRSF1A. GSK1995057 selectively binds to TNFR1, blocks the binding of TNF-α and LT-α, and does not interfere with TNFR2 signaling. GSK1995057 inhibits the activation of NF-κB, JNK and MAPK pathways, alleviates apoptosis (apoptosis) and inflammatory responses (inhibiting IL-1β, IL-6, IL-10, TNF-α), and prevents viability loss of human nucleus pulposus cells. GSK1995057 inhibits the expression of cytokines and neutrophil adhesion molecules in human pulmonary microvascular endothelial cell monolayers, and reduces inflammatory responses and lung injury symptoms in non-human primates. GSK1995057 forms complexes with HAVH autoantibodies, thereby activating TNFR1 and triggering the release of cytokines and IL-8 in human cells. GSK1995057 can be used in research related to intervertebral disc degeneration and acute lung injury .
Vixticibart (REGN-5381) is a fully human IgG4 monoclonal antibody and NPR1 agonist that targets NPR1. Vixticibart stabilizes the receptor in an activated conformation by binding to the N-terminal domain of NPR1, and enhances the activity of endogenous ligands ANP and BNP without blocking ligand binding when these ligands are present. Vixticibart exerts vasodilatory and hypotensive effects by inducing cGMP production, preferentially dilating venous vessels to reduce systolic and venous pressure, but does not induce diuresis and may trigger a compensatory increase in heart rate. Vixticibart produces a synergistic hypotensive effect when combined with angiotensin-converting enzyme inhibitors or angiotensin receptor blockers, and is currently mainly used in research related to heart failure and hypertension .
Denecimig (Mim8) is a factor VIII-mimetic bispecific antibody with micromolar human binding affinity for Factor X and Factor IXa. Denecimig binds Factor X and Factor IXa, localizes both to the phospholipid surface, enhances the Factor IXa-mediated activation of Factor X to Factor Xa, and stimulates the proteolytic activity of Factor IXa via its monovalent anti-Factor IXa arm. Denecimig is applicable to research related to hemophilia A.
Anzurstobart is a CD47/SIRPα inhibitor with human SIRPα Kd of 0.0541 nM and human SIRPα IC50 of 100 nM.Anzurstobart binds SIRPα at a CD47-overlapping site, blocks CD47-SIRPα interactions, inhibits CD47-SIRPα axis signaling, and binds across 6 prevalent human SIRPα haplotypes.Anzurstobart binds SIRPγ and inhibits CD47-SIRPγ interactions.Anzurstobart can be used for the research of non-Hodgkin's lymphoma, colorectal cancer, squamous cell carcinoma of the head and neck, diffuse large B-cell lymphoma, and advanced solid and hematologic malignancies .
Quetmolimab (E6011) is a humanized anti-Fractalkine (CX3CL1) monoclonal antibody. Quetmolimab binds to membrane-bound and soluble Fractalkine, neutralizes Fractalkine-induced migration of CX3CR1-expressing cells, mediates target-bound complex elimination from serum. Quetmolimab suppresses free soluble Fractalkine levels in cynomolgus monkeys, with target engagement linked to increased serum total Fractalkine concentration. Quetmolimab can be used for the research of Crohn’s disease, rheumatoid arthritis, and primary biliary cholangitis .
Anrukinzumab (IMA-638) is a humanized anti-IL-13 monoclonal antibody. Anrukinzumab effectively reduces lung inflammation in a cynomolgus monkey model. Anrukinzumab can be used in studies of ulcerative colitis (UC) as well as asthma .
Pozelimab (REGN3918) is a fully human IgG4 anti-C5 monoclonal antibody. Pozelimab binds to C5 and C5 variants with high affinity and blocks complement-mediated hemolysis. Pozelimab can be used for the research of complement-mediated diseases .
Lanadelumab (SHP643) is a human IgG1 monoclonal antibody against plasma kallikrein (pKal) with an Ki value of 0.12 nM. Lanadelumab inhibits both free and HMWK (high molecular weight kininogen)-bound pKal. Lanadelumab has the potential for the research of hereditary angioedema .
Grisnilimab (WT1) is an IgG2a monoclonal antibody targeting CD7. Grisnilimab only binds to lymphoid tissues and T lymphocytes, with no off-target binding to normal tissues. Grisnilimab can be used to synthesize the immunotoxin WT1-SMPT-dgRTA, which exerts cytotoxic effects on T-lymphoblastic leukemia cells. Grisnilimab is applicable to relevant research on leukemia .
Sasanlimab is a humanized IgG4 isotype anti-PD-1 antibody. Sasanlimab blocks PD-1 interaction with PD-L1/PD-L2, reverses PD-1-mediated inhibitory T-cell signaling, augments T-cell proliferation and cytokine production. Sasanlimab inhibits colon adenocarcinoma tumor growth, and accelerates graft-versus-host disease incidence via enhanced T-cell activity. Sasanlimab can be used for the research of cancer, such as bladder cancer and colon adenocarcinoma .
RFB4 is an anti-CD22 monoclonal antibody. RFB4 can be fused with Pseudomonas aeruginosa exotoxin (PE38) via disulfide bonds to construct recombinant immunotoxins, such as RFB4 (dsFv)-PE38. RFB4 is applicable to the research of cancers including lymphoma .
Emirodatamab (AMG-427) is a bispecific T-cell engager (BiTE). Emirodatamab simultaneously binds FLT3 on the surface of acute myeloid leukemia (AML) cells and CD3 on the surface of T cells, thereby precisely recruiting immune effector cells to tumor sites. Emirodatamab potently induces T cell activation, secretion of proinflammatory cytokines (such as IFNγ, TNFα), and specific cytotoxicity, effectively lysing FLT3-positive tumor cells and inhibiting their growth. Emirodatamab not only significantly prolongs survival in mouse xenograft models and eliminates diseased cells in primates, but also exhibits a synergistic enhancement effect when combined with PD-1 blockade therapy. Emirodatamab is used in studies of acute myeloid leukemia, especially relapsed or refractory cases .
REGN-7257 is a humanized monoclonal antibody targeting IL2RG. REGN-7257 blocks the signal transduction induced by common gamma chain (γc) cytokines via the IL2RG chain of the γc cytokine receptor complex. REGN-7257 is applicable for research on immune-mediated diseases and T cell-mediated diseases . Its corresponding isotype control is Human IgG4 kappa, Isotype Control (HY-P99003).
Anti-Monkey/Human CD28 Antibody (CD28.2) is a mouse-derived IgG1 κ type antibody inhibitor, targeting to monkey/human CD28. Anti-Monkey/Human CD28 Antibody (CD28.2) can block CD28 signaling. Anti-Monkey/Human CD28 Antibody (CD28.2) can be used for the research of immunology .
Anti-Monkey/Human MHC class II (HLA-DR) Antibody (L243) is a mouse-derived IgG2a κ type antibody inhibitor, targeting to monkey/human MHC class II. Anti-Monkey/Human MHC class II (HLA-DR) Antibody (L243) can inhibits tumor cells proliferation and induce apoptosis. Anti-Monkey/Human MHC class II (HLA-DR) Antibody (L243) increases cellular reactive oxygen species (ROS) and loss of mitochondrial membrane potential in human endothelial cells. Anti-Monkey/Human MHC class II (HLA-DR) Antibody (L243) can be used for the researches of cancer and infection, such as lymphoma .
Anti-Monkey/Human CD40L/CD154 Antibody (5C8) is a mouse-derived IgG2a type antibody inhibitor, targeting to monkey/human CD40L/CD154. Anti-Monkey/Human CD40L/CD154 Antibody (5C8) blocks the interactionbetween CD154 and CD40. Anti-Monkey/Human CD40L/CD154 Antibody (5C8) can be used for the researches of inflammation and immunology, such as colitis and transplant .
Cudarolimab (IBI101) is a completely human anti-OX40 (CD134, a co stimulating molecule expressed by activated immune cells) antibody. Cudarolimab inhibits the binding of OX40 to its ligand OX40L. Cudarolimab has antitumor activity and can be used in cancer related research .
Inclacumab (Anti-Human selectin P Recombinant Antibody) is a human monoclonal IgG4 antibody selectively targets P-selectin with a Kd value of 9.9 nM. Inclacumab inhibits P-selectin glycoprotein ligand 1 (PSGL-1) mimetic peptide bind with P-selectin with an IC50 value of 1.9 μg/mL and strongly inhibits cell adhesion .
Veligrotug (AVE1642) is a selective, fully human IGF-1R antagonist antibody with a Kd value of 0.55 nM for hIGF-1R. Veligrotug blocks the phosphorylation of downstream AKT. Veligrotug is applicable to research related to thyroid eye disease .
Spartalizumab is a humanized PD-1 IgG4 monoclonal antibody, with a Kd of 0.83 nM for human PD-1 and a Kd of 0.93 nM for cynomolgus monkeyPD-1. Spartalizumab binds to PD-1 and blocks its interaction with the ligands PD-L1 and PD-L2. Spartalizumab induces increased IFNγ release. Spartalizumab can be used in the research of anaplastic thyroid carcinoma (ATC) and neuroendocrine neoplasms (NENs) .
NGM-438 is a humanized monoclonal antibody antagonist of LAIR1, with a Ka of 0.26 nM for human LAIR1 and 4.28 nM for cynomolgus monkeyLAIR1. NGM-438 blocks the binding of LAIR1 to its Collagen ligand and antagonizes the Collagen-induced LAIR1 signaling pathway. NGM-438 reverses FcγR signaling inhibition in myeloid cells, induces dendritic cells to secrete TNFα, promotes T cell proliferation, and triggers myeloid inflammation and allogeneic T cell responses. NGM-438 sensitizes refractory mouse lung cancer to PD-1 blockade, increases the content of intratumoral CD8 + T cells and the expression of inflammatory genes. NGM-438 is applicable to research related to solid tumors, refractory solid tumors and non-small cell lung cancer .
Zubotamig (Gen1047) is an CD3E/VTCN1-targeting Ig(G1 -κ_G1 -λ2) type chimeric human antibody. The recommed isotype control is Human IgG1 kappa, Isotype Control (HY-P99001). Zubotamig induces T-cell mediated cytotoxicity of B7H4-positive tumor cells, triggers T-cell activation, and induces cytokine release from T cells in the presence of B7H4-expressing tumor cells. Zubotamig demonstrates antitumor activity in mouse patient-derived xenograft (PDX) models. Zubotamig can be used for the research of solid cancers (including breast, ovarian and lung cancer) .
Anti-Monkey/Human MDR-1/CD243 Antibody (UIC2) is an anti-monkey/human MDR-1/CD243 IgG2a monoclonal antibody. Anti-Monkey/Human MDR-1/CD243 Antibody (UIC2) can efficiently inhibit P-glycoprotein. Anti-Monkey/Human MDR-1/CD243 Antibody (UIC2) enhances the inhibitory effect on multidrug resistance (MDR) by suppressing drug efflux. Anti-Monkey/Human MDR-1/CD243 Antibody (UIC2) can be used for research on cancer .
Suvizumab (KD-247) is an neutralizing antibody anti-HIV-1. Suvizumab effectively neutralizes HIV-1MN, HIV-1SF2 and HIV-189.6 with IC50 values of 0.1 µg/mL, 1.0 µg/mL and 0.2 µg/mL, respectively. Suvizumab reduces the viral load of HIV. Suvizumab has good tolerance and can be used to prevent HIV infection .
Anti-Monkey/Human CD20 Antibody (2H7) is a mouse-derived IgG2b κ type antibody inhibitor, targeting to monkey/human CD20. Anti-Monkey/Human CD20 Antibody (2H7) specifically depletes B cells. Anti-Monkey/Human CD20 Antibody (2H7) can be used for the researches of inflammation and metabolic disease, such as diabetes and experimental autoimmune encephalomyelitis .
Visugromab (CTL-002) (Powder) is a GDF-15 neutralizing IgG4 mAb. Visugromab (Powder) has synergistic anticancer activity with the anti-PD1 antibody Nivolumab (HY-P9903) and can effectively act on PD-1/PD-L1 relapsed/refractory metastatic solid tumors. Recommend Isotype Controls: Human IgG4 (S228P) kappa, Isotype Control (HY-P99003) .
Imvotamab (IGM-2323) is a CD20 and CD3 bispecific IGM antibody with dual action mechanism. Imvotamab is used to induce physiological T cell activation to prevent over-stimulation and subsequent down-regulation of immune function. Imvotamab can be used for the study of B-cell malignant tumors, multiple myeloma (MM) and non-Hodgkin's lymphoma (NHL) .
Gentulizumab (Gensci-059) is a humanized IgG4 antibody that targets CD47. Gentulizumab displays strong binding to CD47 in both human and monkey, and effectively inhibits the CD47-SIRPα interaction. Gentulizumab exhibits a potent antitumor activity. The isotype control for Gentulizumab can refer to Human IgG4 (S228P) kappa, Isotype Control (HY-P99003) .
AMG-424 (XmAb968) is a human bispecific antibody (bsAb) targeting CD38 & CD3E. AMG-424 kills CD38-expressing cancer cells, triggers T-cell proliferation and attenuates cytokine release. AMG 424 has antitumor activity in a bone marrow-invasive mouse cancer model and induces peripheral B-cell depletion in cynomolgus monkeys. AMG-424 can be used in multiple myeloma research. Recommended isotype control: half-IG G1-kappa/(scFv-heavy-lambda)-h-CH2-CH3 .
Itanistomig (LB-101) is a tetravalent bispecific antibody targeting PD-L1 and CD47. Itanistomig blocks PD-L1 and achieves tumor enrichment through binding to PD-L1, and also exerts conditional CD47 blocking activity via cleavage of the hinge linker in the PD-L1-positive tumor microenvironment. Itanistomig induces antibody-dependent cellular phagocytosis in human CD14 + cells and drives tumor regression. Itanistomig can be used in research related to solid tumors .
Amtabafusp alfa (GS-8588) is an envelope-targeting bispecific T-cell engager for HIV treatment. Amtabafusp alfa redirects effector T cells by binding to CD3 via a humanized anti-CD3 Fab domain and to HIV envelope proteins via an engineered CD4 domain 1 variant. Amtabafusp alfa exhibits potent, broad-spectrum activity against a variety of HIV isolates and specifically kills HIV-infected cells. Amtabafusp alfa can be used for research on HIV infection .
Anti-Mouse/Rat/Monkey/Human ICOS/CD278 Antibody (C398.4A) is an anti-mouse/rat/monkey/human ICOS/CD278 IgG monoclonal antibody. Anti-Mouse/Rat/Monkey/Human ICOS/CD278 Antibody (C398.4A) has limited effectiveness in improving T cell function and immune activation. Anti-Mouse/Rat/Monkey/Human ICOS/CD278 Antibody (C398.4A) can be used for researches on cancer and infection conditions such as gliomas and hepatitis B virus infection .
MT204 is a humanized IgG1 antibody inhibitor targeting IL-2 of human and rhesus monkey origin. MT204 prevents soluble IL-2 from binding to intermediate-affinity IL-2 receptors and blocks CD25-bound IL-2 on high-affinity IL-2 receptors. MT204 has potently anti-proliferative activity with NKL cells and primary NK cells. MT204 has good tolerability and potent immunosuppressive activity in allogeneic skin graft model of rhesus monkey, promising for immunosuppressive and anti-proliferative therapy .
Ogalvibart (C-135-LS) is a human anti-SARS-CoV-2 monoclonal antibody (IgG1 type). Ogalvibart binds to the spike (S) glycoprotein receptor-binding domain (RBD) of SARS-CoV-2. Ogalvibart in combination with C144LS (1:1 ratio) shows good preventive activity and can effectively block the development of COVID19 in a rhesus monkey disease model .
Anti-Human/Monkey NKG2D Antibody (ON72) is an antibody targeting human/monkeyNKG2D. The isotype control for Anti-Human/Monkey NKG2D Antibody (ON72) can be referenced as Mouse IgG1 kappa, Isotype Control (HY-P99977).
Anti-Human/Monkey NKG2D Antibody (16F16) is an antibody targeting human/monkeyNKG2D. The isotype control for Anti-Human/Monkey NKG2D Antibody (16F16) can be referenced as Human IgG4 kappa, Isotype Control (HY-P99003).
Anti-Human/Monkey CXCR4 Antibody (12G5) reacts with human and monkey CXCR4. Anti-Human/Monkey CXCR4 Antibody (12G5) blocks the cognate ligand, CXCL12/SDF-1, and gp120/160 from binding to CXCR4. Recommend Isotype Controls: Mouse IgG2a kappa, Isotype Control (HY-P99978) .
Anti-Human/Monkey CD16a Antibody (3G8) is a monoclonal antibody targeting CD16a. Anti-Human/Monkey CD16a Antibody (3G8) blocks FcγRIII/CD16a, upregulates the metabolic activity of CD16+ cells, downregulates CD87, a poor prognostic marker, and inhibits the engraftment and growth of leukemia cells in acute myeloid leukemia, and rapidly increases platelet counts in immune thrombocytopenia. Anti-Human/Monkey CD16a Antibody (3G8) is applicable to research related to tumor immunology .
Anti-Human/Mouse/Monkey CXCR3 Antibody (9C5) is an antibody targeting CXCR3, which specifically binds to an epitope within amino acid residues 23 to 44 of human CXCR3 .
TPP-9476 is an anti-human IL3RA (CD123) monoclonal antibody with human IL3RAKd of 11 nM and cynomolgus monkeyIL3RAKd of 16 nM. TPP-9476 binds specifically to human and cynomolgus monkeyIL3RA, undergoes target-dependent internalization into lysosomes of IL3RA-positive cells.TPP-9476 exerts antiproliferative effects in IL3RA-expressing acute myeloid leukemia and classical Hodgkin lymphoma cells, reduces tumor burden, improves survival, and induces complete tumor remission in relevant xenograft mouse models .
AMY109 is an anti-human interleukin-8 (IL-8) monoclonal antibody, with IC50 values of 0.14 μg/mL and 0.37 μg/mL against human IL-8, a Ka of 36.8 pM for human IL-8, and a Ka of 380 pM for cynomolgus monkey IL-8.\nAMY109 binds to human and cynomolgus monkey IL-8 in a pH-dependent manner, inhibits IL-8-mediated activation of CXCR1 and CXCR2, and blocks the downstream biological activities of IL-8. AMY109 inhibits neutrophil recruitment to endometriotic lesions and suppresses monocyte chemoattractant protein-1 production by neutrophils. AMY109 is applicable to research related to endometriosis .
GSK2394002 is an antibody inhibitor targeting ADAMTS-4 and ADAMTS-5, with cartilage-penetrating ability following systemic administration. GSK2394002 inhibits the release of aggrecan-derived neoepitopes and reduces cartilage degradation, exhibiting the potential to relieve pain, alleviate hyperalgesia and inhibit the progression of joint damage. GSK2394002 also induces potentially irreversible cardiovascular effects such as increased mean arterial pressure and myocardial ischemia in cynomolgus monkeys .
HZD37-5 is a humanized monoclonal antibody specifically recognizing N78 loci of IL-17A. HZD37-5 binds to human and rhesus monkeys, blocks IL-17 induced signal transduction and the release of IL-6, IL-8, CXCL-1 and GM-GSF.HZD37-5 significantly inhibited human IL-17A induced-keratinocyte chemoattractant secretion. HZD37-5 can be used for the research of autoimmune diseases including psoriasis and psoriatic arthritis .
IBI352g4a is a humanized IgG1 monoclonal antibody targeting PVRIG (Kd = 0.53 nM) and acts as a PVRIG/PVRL2 inhibitor. The anti-tumor effect of IBI352g4a depends on the binding of its Fc region to FcγR. IBI352g4a binds to the extracellular domains of human and cynomolgus monkey PVRIG, and blocks the PVRIG-PVRL2 interaction. IBI352g4a induces NK cell activation, promotes their degranulation and tumor killing. IBI352g4a can be used in the research of gastric cancer .
RC98 is a monoclonal antibody targeting programmed cell death ligand 1 (PD-L1) and acts as a selective PD-L1 inhibitor. RC98 binds specifically to human and cynomolgus monkey PD-L1. RC98 blocks the interaction between PD-L1 and its receptor PD-1 to reverse T-cell inactivation mediated by PD-1/PD-L1 signaling. RC98 enhances the cytotoxic T-lymphocyte-mediated anti-tumor immune response against PD-L1-expressing tumor cells. RC98 can be used for the research of tumor immunity and solid tumors .
PF-03475952 is a fully human IgG2 monoclonal antibody targeting CD44. PF-03475952 binds an epitope in CD44’s constant exons, blocks CD44-hyaluronic acid interaction, reduces cell surface CD44, and does not cross-react with rodent CD44 or LYVE-1. PF-03475952 induces cancer cell apoptosis, inhibits LPS (HY-D1056)-induced leukocyte cytokine release and cancer metastasis, and reduces CD44 expression on circulating CD3+ lymphocytes in cynomolgus monkeys. PF-03475952 can be used for the research of rheumatoid arthritis and hepatocellular carcinoma .
SK48-E26 is a human interleukin-1β (IL-1β) inhibitor, with a IC50 of 400 pM against human IL-1β, a IC50 of 185 pM against cynomolgus monkey IL-1β, and a Ka value ranging from 0.048 nM to 3 nM for human IL-1β. SK48-E26 binds to the conformational epitope of human IL-1β spanning amino acid residues 95-101, and blocks the biological activity of IL-1β. SK48-E26 can be used in research related to IL-1β-mediated inflammatory diseases and osteoarthritis .
Arevirumab (Arevirumab-3) is a pan-lineage neutralizing human monoclonal antibody cocktail (8.9F, 12.1F, 37.D). Arevirumab protects cynomolgus monkeys from severe Lassa fever caused by lineage II and III LASV isolates. Arevirumab is applicable to research related to Lassa fever .
GNUV201 is a PD-1 inhibitor with cross-reactivity in humans, mice and monkeys, which effectively blocks the PD-1/PD-L1 interaction. GNUV201 activates T cells and restores their anti-tumor activity, effectively inducing tumor regression. GNUV201 can be used in the research of related diseases such as colorectal cancer, melanoma, pancreatic cancer and colon cancer .
REGN4659 is a fully human anti-CTLA-4 monoclonal antibody and IgG1 antibody. REGN4659 binds to the extracellular domain of human and monkey CTLA-4 with high affinity and specificity. REGN4659 blocks CTLA-4 interaction with CD80 and CD86 ligands. REGN4659 significantly suppresses MC38.Ova tumor growth in CTLA-4 knock-in mice .
LY3541860 is a selective anti-CD19 antibody that both binds human CD19 with high affinity and selectively binds human B cells (Kd values: 76.8 pM and 94.5 nM for humans and cynomolgus monkeys, respectively). LY3541860 inhibits CpG-induced CD69 expression (IC50 = 0.006 nM). LY3541860 exhibits potent B cell inhibitory activities. LY3541860 can inhibit both BCR- and TLR-induced human B cell activation. LY3541860 can be used for the research of autoimmune diseases .
AS3288802, a highly selective active plasminogen activator inhibitor-1 (PAI-1) antibody, is a PAI-1 inhibitor with a human IC50 and EC50 values of 4.2 ng/mL. AS3288802 can be used for the research of thrombosis and fibrosis-related diseases .
BAY-356, a potent TWEAK receptor agonist, is an aglycosylated anti-TWEAK receptor antibody. BAY-356 triggers TWEAKR hyperactivation, activates NFκB and STAT1 pathways, and undergoes TWEAKR-dependent internalization. BAY-356 can be used for the research of colorectal cancer, bladder cancer, non-small cell lung cancer and pancreatic cancer[1][2].
KHK2840 is a potent CD40 agonist with a Kd value of 0.485 nM for hCD40. KHK2840 delivers agonistic signals in tumor-bearing hCD40 transgenic mice and human peripheral blood B cells. KHK2840 upregulates CD80, CD86, CD95 and IL-12p70 expression. KHK2840 enhances antitumor efficacy of anti-PD-1 antibody and Paclitaxel (HY-B0015). KHK2840 can be used for the research of cancer, such as colon cancer and melanoma .
QX008N is a humanized IgG1 monoclonal antibody and also a TSLP inhibitor with a KD value of 0.0175 nM. QX008N blocks TSLP-induced signaling pathways by inhibiting the interaction of TSLP-TSLPR-IL-7Rα. QX008N reduces eosinophil and IgE levels, improves pulmonary function, blocks TSLP-induced inflammation, and enhances the inhibitory effect on inflammatory mediators when administered in combination with anti-IL-4R antibodies. QX008N is applicable to relevant research on asthma .
SHR-A1403 Antibody is an anti-c-Met monoclonal antibody. SHR-A1403 Antibody down-regulates phosphorylated c-Met, Akt, ERK, weakens intracellular signal cascades, and mediates antibody-c-Met complex endocytosis. SHR-A1403 Antibody can be used for the research of c-met-overexpressing cancers and pancreatic ductal adenocarcinoma .
NMB04 is a recombinant anti-Human CD257 (BAFF) (BLyS) antibody. NMB04 binds with specificity and high affinity to soluble and membrane-bound Blys, and blocks Blys binding to receptors TACI, BCMA, and BR-3. NMB04 can be used for the research of autoimmune diseases .
AVID100 Antibody (MAB100) is a monoclonal antibody inhibitor targeting EGFR, which can be used to synthesize a novel antibody-drug conjugate (ADC) molecule AVID100. AVID100 Antibody is applicable to relevant research on breast cancer, head and neck cancer, and lung cancer .
SOT102 Antibody is an IgG1 monoclonal antibody targeting CLDN18.2. SOT102 Antibody binds selectively to CLDN18.2, and promotes internalization. SOT102 Antibody can be used for the research of cancer [2].
APG808 is an anti-human IL-4Rα monoclonal antibody. APG808 binds to IL-4Rα, prevents IL-13Rα1/IL-4Rα heterodimer formation, and disrupts IL-13 and IL-4 mediated signaling. APG808 ablates Fc and complement effector functions. APG808 can be used for the research of chronic obstructive pulmonary disease, asthma, atopic dermatitis .
PF-06650808 Antibody (Anti-NOTCH3 mAb hu28) is an IgG1-kappa Notch3-targeting antibody. PF-06650808 Antibody is the antibody component of the antibody-drug conjugate (ADC) PF-06650808. PF-06650808 Antibody can be used for the research of advanced breast cancer, advanced solid tumors .
DB-1310 Antibody is a monoclonal antibody inhibitor targeting HER3. DB-1310 Antibody can be used to synthesize the antibody-drug conjugate (ADC) DB-1310. DB-1310 Antibody is applicable to research related to HER3-positive solid tumors, non-small cell lung cancer, breast cancer, colon cancer and prostate cancer .
LR004 is an EGFR monoclonal antibody, with a Kd of 2.80 × 10 -9 M against human EGFR. LR004 shows extremely weak inhibitory effect on the viability of EGFR-positive tumor cells in vitro, but inhibits the growth of EGFR-positive tumor xenografts as a single agent. LR004 is applicable to research related to advanced colorectal cancer, solid tumors, esophageal squamous cell carcinoma, epidermoid carcinoma, colon cancer and breast cancer .
SAR-443809 is a selective alternative complement system inhibitor and monoclonal antibody targeting complement factor Bb. SAR-443809 blocks the cleavage of C3 and factor B by selectively binding to the activated form of factor Bb, with a KD of 7.3 nM for human factor Bb. SAR-443809 inhibits the amplification loop of the alternative complement pathway and C3 activation, reduces C3b deposition, and blocks the activation of pathways associated with intravascular and extravascular hemolysis. SAR-443809 can be used for the research of hematological and renal disorders mediated by abnormal alternative complement pathway .
JNJ-55920839 (CNTO-6358) is a fully human immunoglobulin G1κ monoclonal antibody and a selective Interferonα/ω neutralizer, with a Kd value of 0.9-10.7 pM against hIFNα and a Kd of 1.44 pM against IFNω. JNJ-55920839 can be used in research related to systemic lupus erythematosus .
SHR-2010 is a fully humanized monoclonal antibody targeting MASP-2. SHR-2010 selectively inhibits lectin pathway activation without affecting classical or alternative complement pathways. SHR-2010 can be used for the research of IgA nephropathy .
PF-06817024 is a high affinity, humanized antibody that binds IL-33. PF-06817024 binds to IL-33, prevents IL-33 from binding to receptor ST2, and inhibits downstream type 2 inflammatory responses. PF-06817024 can be used for the research of allergic diseases .
SHR-1802 is a humanized anti-LAG-3 monoclonal antibody.SHR-1802 specifically binds to LAG-3 and inhibits its binding to major histocompatibility complex class II (MHC-II), fibrinogen-like protein 1 (FGL1), galectin-3, and liver sinusoidal endothelial cell lectin.SHR-1802 can be used for the research of advanced solid tumors .
Anti-Human/Mouse LY6E Antibody (9B12) is a high-affinity, multi-target antibody that binds specifically to LY6E. Anti-Human/Mouse LY6E Antibody (9B12) binds specifically to cell-surface LY6E and enters lysosomes via lipid raft-dependent endocytosis, thereby effectively inhibiting the growth of various LY6E-expressing solid tumors (such as breast cancer and lung cancer) in both in vitro and in vivo models. Anti-Human/Mouse LY6E Antibody (9B12) exerts a dual mechanism of action: on one hand, it blocks the interaction between PILRα and CD8α, specifically reduces the survival rate of peripheral CD8 + T cells and induces their activation, breaking the state of cellular quiescence; on the other hand, it recognizes and immunoprecipitates IDE under both non-denaturing and denaturing conditions, which is applicable to studies on the subcellular localization and protein interactions of IDE. The regulatory effect of Anti-Human/Mouse LY6E Antibody (9B12) on CD8 + T cells strictly depends on the presence of PILRα, and it does not affect CD4 + T cells or T cell development in the thymus, exhibiting high specificity .
TNX-1500 is a crystallizable fragment-modified anti-CD154 antibody. TNX-1500 contains the hu5c8 fragment antigen-binding (Fab) domain from Ruplizumab (HY-P99315) and an IgG4 Fc region engineered to reduce FcγRIIa binding. TNX-1500 has significantly weaker binding affinity to FcγRI, FcγRIIaH, FcγRIIbF, FcγRIIIaF, and FcγRIIIaV compared to hu5c8 (Kdvalues: 8.7 nM, 7100 nM, 4900 nM, 8000 nM, 6000 nM respectively). TNX-1500 prolongs nonhuman primate renal allograft survival, prolongs nonhuman primate cardiac allograft survival. TNX-1500 can be used for the research of allograft rejection [1][2].
Digitoxin is an anti-cancer agent. Digitoxin induces apoptosis, inhibits influenza cytokine storm, causes DNA double-stranded breaks (DSBs) and blocks the cell cycle at the G2/M phase. Digitoxin induces calcium uptake into cells by forming transmembrane calcium channels and can be used for research of heart failure .
Cholesteryl oleate is an ester compound formed from Cholesterol (HY-N0322) and Oleic acid (HY-N1446), which is involved in lipid transport, storage and cell membrane formation in living organisms. Cholesteryl oleate may serve as a potential biomarker for prostate cancer. Cholesteryl oleate can also prepare cationic solid lipid nanoparticles (SLNs) for efficient gene silencing .
7-Methylxanthine is an orally active methyl derivative of xanthine and a non-selective adenosine receptor antagonist. 7-Methylxanthine is also one of the purine components of human urinary calculi. 7-Methylxanthine has anti-myopia activity .
Artemotil (β-Arteether) has antimalarial activity for the treatment of chloroquine-resistant Plasmodium falciparum malaria with an IC50 of 1.61 nM. Artemotil also has central nervous system (CNS) neurotoxicity and anorectic toxicity in rats, dogs and monkeys .
7-Ethoxycoumarin is a substrate of cytochrome P450 (CYP450). 7-Ethoxycoumarin has been used for the functional characterization of various CYPs and for the generation of 7-hydroxycoumarin (HY-N0573) .
Ancitabine hydrochloride is a cytarabine derivative that inhibits viral replication. Ancitabine hydrochloride blocks vaccinia virus DNA replication, the progression of viral protein synthesis from early to late stages, and one-step growth of vaccinia virus. Ancitabine hydrochloride is applicable to research related to vaccinia virus infection, leukemia, human cytomegalovirus infection and colorectal cancer .
L-Alanyl-L-leucine is a competitive inhibitor of small intestinal glycyl-L-leucine hydrolase with Ki values of 0.53 mM (phosphate buffer) or 0.22 mM (Tris buffer). L-Alanyl-L-leucine can be used for research on Hartnup disease and cystinuria .
Cubebin ((-)-Cubebin), a dibenzyl butyrolactone lignan, is an orally active AChE inhibitor. Cubebin binds to active sites of NF-κB, TNF-α, and TGF-β1 via hydrogen and hydrophobic interactions, obstructing critical residues to inhibit pro-inflammatory or renal fibrosis-related activity. Cubebin enhances p38 MAPK phosphorylation to increase tyrosinase gene expression, stimulating melanogenesis via elevated tyrosinase activity, expression, and mRNA levels. Cubebin reduces oxidative stress via enhanced endogenous antioxidant enzyme activity and inhibited lipid peroxidation, regulates lipid metabolism, improves glycemic control, and exerts renoprotective effects via reduced renal dysfunction markers and improved renal architecture. Cubebin shows antimicrobial activity. Cubebin exerts larvicidal activity against Angiostrongylus cantonensis larvae, with no cytotoxicity toward monkey or human cell lines or Caenorhabditis elegans. Cubebin can be used for the research of diabetic nephropathy, melanoma, colon adenocarcinoma, neuroangiostrongyliasis, Alzheimer’s disease (AD) and depression .
Guanfu base A is an antiarrhythmic alkaloid isolated from Aconitum coreanum and is a potent noncompetitive CYP2D6 inhibitor, with a Ki of 1.20 μM in human liver microsomes (HLMs) and a Ki of 0.37 μM for the human recombinant form (rCYP2D6). Guanfu base A is also a potent competitive inhibitor of CYP2D in monkey (Ki of 0.38 μM) and dog (Ki of 2.4 μM) microsomes . Guanfu base A also inhibits HERG channel current .
L-Alanyl-L-leucine is an endogenous metabolite. This product is used for research and analytical applications. L-Alanyl-L-leucine is a competitive inhibitor of small intestinal glycyl-L-leucine hydrolase with Ki values of 0.53 mM (phosphate buffer) or 0.22 mM (Tris buffer). L-Alanyl-L-leucine can be used for research on Hartnup disease and cystinuria .
Digitoxin (Standard) is the analytical standard of Digitoxin. This product is intended for research and analytical applications. Digitoxin is an anti-cancer agent. Digitoxin induces apoptosis, inhibits influenza cytokine storm, causes DNA double-stranded breaks (DSBs) and blocks the cell cycle at the G2/M phase. Digitoxin induces calcium uptake into cells by forming transmembrane calcium channels and can be used for research of heart failure .
4-Hydroxymethylpyrazole is the primary metabolite of Fomepizole (HY-B0876) produced through hepatic oxidative metabolism. 4-Hydroxymethylpyrazole exhibits a plasma concentration that is positively correlated with the administered dosage of Fomepizole, and it demonstrates a relatively short half-life. 4-Hydroxymethylpyrazole demonstrates inhibitory effects on alcohol dehydrogenase (ADH) in both humans and monkeys, but its inhibition constant is significantly higher than that of Fomepizole, rendering its in vivo impact negligible .
7-Ethoxycoumarin (Standard) is the analytical standard of 7-Ethoxycoumarin. This product is intended for research and analytical applications. 7-Ethoxycoumarin is a substrate of cytochrome P450 (CYP450). 7-Ethoxycoumarin has been used for the functional characterization of various CYPs and for the generation of 7-hydroxycoumarin (HY-N0573) .
Isoxepac (Standard) is the analytical standard of Isoxepac. This product is intended for research and analytical applications. Isoxepac (HP 549) is a nonsteroidal anti-inflammatory agent (NSAID) with anti-inflammatory, analgesic and antipyretic activity. Isoxepac has been studied in rat, rabbit, dog, rhesus monkey, etc .
Guanfu base A hydrochloride is an antiarrhythmic alkaloid with the ability to inhibit CYP2D6 enzyme activity. Guanfu base A hydrochloride can be used to inhibit arrhythmia-related diseases. Guanfu base A hydrochloride exhibits inhibitory effects on CYP2D6 in different species of organisms, including humans, monkeys, and dogs. The biological activity of Guanfu base A hydrochloride makes it have potential clinical application value .
4-Hydroxymethylpyrazole (Standard) is an analytical standard for 4-Hydroxymethylpyrazole (HY-33914). This product is intended for research and analytical applications. 4-Hydroxymethylpyrazole is the primary metabolite of fomepizole (HY-B0876) via hepatic oxidative metabolism. 4-Hydroxymethylpyrazole exhibits a plasma concentration that is positively correlated with the administered dosage of Fomepizole, and it demonstrates a relatively short half-life. 4-Hydroxymethylpyrazole inhibits alcohol dehydrogenase (ADH) in humans and monkeys, but the inhibition constant is much higher than that of fomepizole and is therefore negligible in vivo
Relugolix-d6 is deuterium labeled Relugolix. Relugolix (TAK-385)?is a potent, orally active, nonpeptidic gonadotropin-releasing hormone (GnRH) antagonist. Relugolix possesses high affinity 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 .
Ubrogepant-d5 (MK-1602-d5) is deuterium labeled Ubrogepant. Ubrogepant (MK-1602) is an orally active and selective antagonist of calcitonin gene-related peptide receptor (CGRP). Ubrogepant has high affinity for CGRP receptors in human and rhesus monkeys, and can effectively block the cAMP response stimulated by α-CGRP. Ubrogepant can be used in the study of acute migraine .
Hydroxyprogesterone caproate-d8 (17α-Hydroxyprogesterone hexanoate-d8) is the deuterium labeled Hydroxyprogesterone caproate (HY-B0742). Hydroxyprogesterone caproate (17α-Hydroxyprogesterone hexanoate; 17α-Hydroxyprogesterone caproate) is a progesterone receptor (progesterone receptor) ligand and steroid hormone transcription inhibitor. Hydroxyprogesterone caproate downregulates estrogen receptors in target tissues and activates their metabolic pathways, and exhibits equivalent affinity for progesterone receptor A and progesterone receptor B. Hydroxyprogesterone caproate shows no consistent teratogenicity or developmental toxicity in rat, mouse and monkey models, but induces resorption or abortion in rhesus monkeys at human-equivalent doses. Hydroxyprogesterone caproate promotes the production of TNF-α in lipopolysaccharide-stimulated whole blood from non-pregnant women. Hydroxyprogesterone caproate can be used in scientific research related to preterm birth .
5-Hydroxy saxagliptin- 13C,d2-2 hydrochloride is the 13C- and deuterium labeled 5-Hydroxy saxagliptin hydrochloride. 5-Hydroxy saxagliptin hydrochloride is an active metabolite of Saxagliptin (HY-10285) and a potent and selective DPP-4 inhibitor. 5-Hydroxy saxagliptin hydrochloride has Ki values of 2.6 nM and 2.9 nM for humans and cynomolgus monkeys, respectively. 5-Hydroxy saxagliptin hydrochloride can be used in the research of type 2 diabetes mellitus .
Human, Mouse, Monkey, Goat, Hamster, Rat, Chlamydomonas Reinhardtii
Beta Tubulin Antibody (YA839) is a non-conjugated and Mouse origined IgG1 monoclonal antibody, targeting to Tubulin beta chain (TUBB). It can be used as a loading control antibody.
A-62198 is a potent and selective renin inhibitor with antihypertensive activity. A-62198 reduces mean arterial pressure (MAP) in anesthetized, salt-deprived monkeys in a dose-dependent manner. A-62198 induced MAP reduction in normal monkeys that reached statistical significance at the highest dose and significantly inhibited plasma renin activity (PRA) at all doses .
Cholesteryl oleate is an ester compound formed from Cholesterol (HY-N0322) and Oleic acid (HY-N1446), which is involved in lipid transport, storage and cell membrane formation in living organisms. Cholesteryl oleate may serve as a potential biomarker for prostate cancer. Cholesteryl oleate can also prepare cationic solid lipid nanoparticles (SLNs) for efficient gene silencing .
Givosiran (ALN-AS1) sodium is a small interfering RNA that targets hepatic aminolevulinate synthase 1 (ALAS1) messenger RNA. Givosiran sodium downregulates ALAS1 mRNA and prevents accumulation of neurotoxic δ-aminolevulinic acid (ALA) and porphobilinogen (PBG) levels. Givosiran sodium demonstrates potent inhibitory activity against ALAS1 in mouse, rat, and cynomolgus monkey models. Givosiran sodium can be used for the research of acute hepatic porphyria (AHP) .
Givosiran (ALN-AS1) is a small interfering RNA that targets hepatic aminolevulinate synthase 1 (ALAS1) messenger RNA. Givosiran downregulates ALAS1 mRNA and prevents accumulation of neurotoxic δ-aminolevulinic acid (ALA) and porphobilinogen (PBG) levels. Givosiran demonstrates potent inhibitory activity against ALAS1 in mouse, rat, and cynomolgus monkey models. Givosiran can be used for the research of acute hepatic porphyria (AHP) .
Inotersen (GSK-2998728; ISIS-420915) is a 2'-O-methoxyethyl-modified antisense oligonucleotide and transthyretin (TTR) inhibitor with low genotoxicity. Inotersen triggers RNase H1-mediated degradation by binding to TTR mRNA, thereby effectively reducing the production of both mutant and wild-type transthyretin in the liver. Inotersen significantly reduces amyloid fiber deposition, yet specific toxicities such as inflammation or tumors are observed at high doses in some animal models. Inotersen is used in studies of hereditary transthyretin amyloidosis and the associated polyneuropathy and cardiomyopathy .
Rondaptivon pegol (BT200) sodium is an aptamer targeting von Willebrand factor (VWF), with an EC50 of 33 nM in humans. Rondaptivon pegol sodium effectively alleviates acute myocardial ischemia-reperfusion injury in mice by inhibiting VWF activity, reducing microvascular obstruction, inflammatory responses and cardiomyocyte apoptosis (apoptosis). Rondaptivon pegol sodium inhibits the binding of VWF to platelet glycoprotein GPIb, thereby preventing arterial thrombosis in cynomolgus monkeys. Rondaptivon pegol sodium can be used in research related to arterial thrombosis, stroke, myocardial infarction and myocardial ischemia-reperfusion injury .
Rugonersen (RG6091; RO7248824) is a locked-nucleic acid (LNA)- modified antisense oligonucleotides (ASOs), and results in reduction of ubiquitin-protein ligase E3A (UBE3A) silencing. Angelman syndrome (AS) is a severe neurodevelopmental disorder caused by the loss of neuronal E3 ligase UBE3A, Rugonersen has been used for AS reasearch .
Cemdisiran (ALN-CC5) is an N-acetylgalactosamine-conjugated RNAi agent and also a complement component C5 inhibitor. Cemdisiran targets C5 mRNA, cleaves C5 mRNA via the endogenous RNA interference pathway, and inhibits the production of C5 protein in the liver. Cemdisiran exerts a dose-dependent inhibitory effect on total C5 concentrations in cynomolgus monkeys. When used in combination with Pozelimab (HY-P99786) in cynomolgus monkeys, Cemdisiran achieves a more sustained and complete inhibitory effect on complement activity. Cemdisiran can be used in the research of paroxysmal nocturnal hemoglobinuria and other complement-mediated diseases .
Olpasiran (AMG 890, ARC-LPA) sodium is an N-acetyl galactosamine (GalNAc)-conjugated, hepatocyte-targeted siRNA. Olpasiran sodium directly inhibits LPA messenger RNA translation in hepatocytes and potently reduce Lp(a) concentration. Olpasiran sodium can be used for the research of cardiovascular disease, such as atherosclerosis .
ISIS 104838 is an antisense oligonucleotide targeting TNF-α. ISIS 104838 specifically binds to human TNF-α mRNA via Watson-Crick base pairing to form a DNA:RNA hybrid duplex, thereby recruiting the ubiquitously expressed intracellular enzyme RNase H to degrade the target mRNA and inhibit TNF-α protein synthesis at the transcriptional level. ISIS 104838 induces moderate, self-limiting thrombocytopenia in cynomolgus monkeys. ISIS 104838 can be used for the study of inflammatory diseases .
Trecovirsen is an antiviral agent targeting HIV gag mRNA, which hybridizes with complementary HIV gag mRNA at the initiation site. Trecovirsen induces a reversible, dose-dependent prolongation of activated partial thromboplastin time via its polyanionic properties. Trecovirsen is applicable to research related to HIV infection .
ISIS 104838 sodium is an antisense oligonucleotide targeting TNF-α. ISIS 104838 sodium specifically binds to human TNF-α mRNA via Watson-Crick base pairing to form a DNA:RNA hybrid duplex, thereby recruiting the ubiquitously expressed intracellular enzyme RNase H to degrade the target mRNA and inhibit TNF-α protein synthesis at the transcriptional level. ISIS 104838 sodium induces moderate, self-limiting thrombocytopenia in cynomolgus monkeys. ISIS 104838 sodium can be used for the study of inflammatory diseases .
VL-422 is an ionizable cationic lipid. VL-422 delivers CRISPR complementary single-guide RNA (sgRNA) and Cas9 mRNA to enable in vitro and in vivo gene editing. LNPs containing VL-422 loaded with Cas9 mRNA and sgRNA targeting the ANGPTL3 gene induce the deletion of premature stop codons within the ANGPTL3 gene in the liver of cynomolgus monkeys. Loss-of-function of ANGPTL3 leads to decreased levels of LDL, HDL and cholesterol in plasma. The VL-422 delivery system can be used for the research of gene editing strategies targeting lipid metabolism diseases .
Rugonersen sodium is a locked-nucleic acid (LNA)- modified antisense oligonucleotides (ASOs), and results in reduction of ubiquitin-protein ligase E3A (UBE3A) silencing. Angelman syndrome (AS) sodium is a severe neurodevelopmental disorder caused by the loss of neuronal E3 ligase UBE3A, Rugonersen has been used for AS reasearch .
Custirsen (OGX-011) is an antisense oligonucleotide that targets clusterin mRNA. Custirsen induces apoptosis by activating Bax, triggering mitochondrial translocation and cytochrome c release. Custirsen acts as a chemosensitizer, radiosensitizer and hormone sensitizer. Custirsen can be used in research related to prostate cancer, non-small cell lung cancer and metastatic breast cancer .
ATP6V1A Monkey Pre-designed siRNA Set A contains three designed siRNAs for ATP6V1A gene (Monkey), as well as a negative control, a positive control, and a FAM-labeled negative control.
Sgc8c Aptamer is a single-stranded DNA aptamer targeting protein tyrosine kinase 7 (PTK7) with Kd of 1.03-11.73 nM for human, mice, rat and monkey. Sgc8c Aptamer can be used to synthesize aptamer-drug conjugates and can be used for cancer research .
Etedesiran is a component of the AOC drug Delpacibart etedesiran (HY-177565), formed by the reaction of an siRNA that induces cleavage of mRNA encoding myotonic dystrophy protein kinase (MTPK or DMPK) with SMCC linker (HY-42360). Etedesiran carries a maleimide group at its terminus, which can react with cysteine or lysine and is used for the synthesis of AOC drugs. Etedesiran is applicable to research related to myotonic dystrophy type 1 .
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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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