Search Result
Results for "
SHRs
" in MedChemExpress (MCE) Product Catalog:
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-137448
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SHR3680
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Androgen Receptor
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Cancer
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Rezvilutamide (SHR3680) is an androgen receptor antagonist. Rezvilutamide (SHR3680) is used for the study of prostate cancer .
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- HY-151367
-
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ERK
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Cancer
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SHR2415 is a highly potent, selective and orally active ERK1/2 inhibitor. SHR2415 has inhibition activity for ERK1 and ERK2 with IC50 values of 2.8 nM and 5.9 nM, respectively. SHR2415 exhibits high potency with an IC50 value of 44.6 nM in Colo205 cells. SHR2415 can be used for the research of cancer .
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- HY-P99944
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Retlirafusp alfa
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PD-1/PD-L1
TGF-β Receptor
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Cancer
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SHR-1701 (Retlirafusp alfa) is a bifunctional fusion protein targeting PD-L1 and TGF-β for cancer research .
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- HY-104065
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Pyrotinib
Maximum Cited Publications
15 Publications Verification
SHR-1258
|
EGFR
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Cancer
|
Pyrotinib (SHR-1258) is a potent and selective EGFR/HER2 dual inhibitor with IC50s of 13 and 38 nM, respectively .
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- HY-104065B
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SHR-1258 dimaleate
|
EGFR
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Cancer
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Pyrotinib dimaleate (SHR-1258 dimaleate) is a potent and selective EGFR/HER2 dual inhibitor with IC50s of 13 and 38 nM, respectively .
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- HY-P10318
-
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GLP Receptor
|
Endocrinology
|
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 .
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- HY-144319
-
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HBV
|
Infection
|
SHR5133 is a highly potent, orally active HBV capsid assembly modulator. SHR5133 displays HBV DNA reduction (EC50=26.6 nM) .
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- HY-164763
-
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Antibody-Drug Conjugates (ADCs)
EGFR
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Cancer
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SHR-A1201 is a HER2-targeting antibody-drug conjugate (ADC). SHR-A1201 is composed of a humanized anti-HER2 antibody (HY-P9907), a linker SMCC (HY-42360), and a microtubulin inhibitor payload Mertansine (HY-19792). SHR-A1201 can be used for research in HER2-positive breast cancer .
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- HY-104065BR
-
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EGFR
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Cancer
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Pyrotinib dimaleate (Standard) is the analytical standard of Pyrotinib dimaleate. This product is intended for research and analytical applications. Pyrotinib dimaleate (SHR-1258 dimaleate) is a potent and selective EGFR/HER2 dual inhibitor with IC50s of 13 and 38 nM, respectively .
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- HY-144269
-
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Raf
|
Cancer
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SHR902275 is a potent, selective, and orally active RAF inhibitor targeting RAS mutant cancers. SHR902275 has IC50s of 1.6 nM, 10 nM, and 5.7 nM for cRAF, bRAF wt, and bRAF V600E, respectively. SHR902275 shows cell growth inhibition with GI50s of 1.5 and 0.17 nM, 0.4 nM and 0.32 nM for H358, A375, Calu6, and SK-MEL2 cells respectively .
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- HY-114338A
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SHR-6390 hydrochloride
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CDK
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Cancer
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Dalpiciclib (SHR-6390) hydrochloride is an orally active and highly selective inhibitor of CDK4 and 6 with IC50 values of 12.4 nM and 9.9 nM, respectively . Dalpiciclib hydrochloride shows antitumor activity against breast cancer and esophageal squamous cell carcinoma .
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- HY-114338
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SHR-6390
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CDK
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Cancer
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Dalpiciclib (SHR-6390) is an orally active and highly selective inhibitor of CDK4 and 6 with IC50 values of 12.4?nM and 9.9?nM, respectively . Dalpiciclib shows antitumor activity against breast cancer and esophageal squamous cell carcinoma .
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- HY-P99422
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SHR-1316
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PD-1/PD-L1
Apoptosis
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Cancer
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Adebrelimab (SHR-1316) is a humanized IgG4 monoclonal PD-L1 (PD-1/PD-L1) antibody. Adebrelimab has promising antitumor activity in solid tumors including extensive-stage small-cell lung cancer (SCLC) .
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- HY-155787
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CDK
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Cancer
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SHR5428 is a potent, orally active, selective and noncovalent inhibitor of CDK7 with highly potent CDK7 enzymatic activity (IC50=2.3 nM). SHR5428 inhibits triple negative breast cancer cellular activity on MDA-MB-468 cell (IC50=6.6 nM) .
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- HY-P99822
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SHR-1209
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PCSK9
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Metabolic Disease
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Recaticimab (SHR-1209) is a humanized monoclonal antibody that inhibits PCSK9. Recaticimab can bind to PCSK9 and mediate its degradation, increasing the level of low-density lipoprotein (LDL) receptors on the surface of liver cells, reducing the level of LDL in plasma, thereby lowering blood lipids. Recaticimab can be used for the study of hypercholesterolemia .
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- HY-128351
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-
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- HY-115879
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-
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- HY-128355A
-
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Indoleamine 2,3-Dioxygenase (IDO)
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Others
Cancer
|
(R)-IDO/TDO-IN-1 (compound 25) is an indoleamine-2,3-dioxygenase (IDO) inhibitor, with good pharmacokinetic properties. (R)-IDO/TDO-IN-1 exhibits anti-tumor activity in MC38 xenograft model. (R)-IDO/TDO-IN-1 shows synergistic effect with anti-PD-1 monoclonal antibody (SHR-1210) .
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- HY-104065A
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(Rac)-SHR-1258
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Others
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Cancer
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(Rac)-Pyrotinib ((Rac)-SHR-1258) is the racemate of Pyrotinib (HY-104065). Pyrotinib is a potent and selective EGFR/HER2 dual inhibitor.
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- HY-107322A
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Mepirodipine; YM-09730-5 Free base
|
Calcium Channel
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Cardiovascular Disease
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Barnidipine (Mepirodipine) is an L-type calcium antagonist (CaA) with high affinity for [ 3H] initrendipine binding sites (Ki = 0.21 nmol/L), has selective action against CaA receptors. Barnidipine is an orally effective antihypertensive agent that can reduce the level of platelet-derived growth factor B-chain mRNA and peripheral vascular resistance .
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- HY-116262
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Phosphodiesterase (PDE)
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Cardiovascular Disease
Inflammation/Immunology
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SCH 51866 is a potent, selective and orally active inhibitor of PDE1 (IC50=70 nM) and PDE5 (IC50=60 nM). SCH 51866 inhibits collagen-induced aggregation of human washed platelets (IC50=10 μM), prevents neointimal formation in balloon catheter-injured carotid arteries of spontaneously hypertensive rats (SHR), and reduces blood pressure in SHR. SCH 51866 can be used in the study of hypertension .
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- HY-155042
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Angiotensin Receptor
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Cardiovascular Disease
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Antihypertensive agent 3 (compound 4a) is an antagonis of angiotensin II receptor 1. Antihypertensive agent 3 exhibits antihypertensive activity in a spontaneously hypertensive rats (SHRs) model .
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- HY-B1388
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Homatropine methobromide
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mAChR
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Neurological Disease
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Homatropine methylbromide (Homatropine methobromide) is muscarinic AChR antagonist, inhibits endothelial and smooth muscle muscarinic receptors of WKY-E and SHR-E with IC50 of 162.5 nM and 170.3 nM, respectively.
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- HY-153350
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ERK
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Cancer
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ERK-IN-7 (Example 10), an analogue of SHR2415 (HY-151367), is a potent ERK inhibitor with IC50 of 5 nM and 7 nM against ERK1 and ERK2, respectively .
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- HY-121550
-
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Angiotensin-converting Enzyme (ACE)
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Cardiovascular Disease
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ME3221 is an angiotensin AT1 receptor antagonist that effectively antagonizes the pressor response to angiotensin II in rats and marmosets without affecting the hypotensive response to bradykinin. It demonstrates potent antihypertensive effects in renal hypertensive rats and spontaneously hypertensive rats (SHR), with efficacy comparable to or better than losartan in vivo. ME3221's repeated administration in SHR results in sustained and stable hypotensive effects without affecting heart rate, indicating its potential for treating both renal and essential hypertension similarly to losartan .
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- HY-P9971
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SHR-1210
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PD-1/PD-L1
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Cancer
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Camrelizumab (SHR-1210) is a potent humanied high-affinity IgG4-κ monoclonal antibody (mAb) to PD-1. Camrelizumab binds PD-1 at a high affinity of 3 nM and inhibits the binding interaction of PD-1 and PD-L1 with an IC50 of 0.70 nM. Camrelizumab acts as anti-PD-1/PD-L1 agent and can be used for cancer research, including NSCLC, ESCC, Hodgkin lymphoma, and advanced HCC et,al .
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- HY-147408
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SHR9265
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Topoisomerase
ADC Cytotoxin
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Cancer
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Rezetecán (SHR9265) is a topoisomerase I inhibitor. In addition, Rezetecán can be used to synthesize Trastuzumab rezetecan, an antineoplastic agent. Rezetecán can be used as a cytotoxic payload (ADC Cytotoxin) in antibody-drug conjugates (ADCs) .
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- HY-136630
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SHR110008
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Others
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Others
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Felotaxel (SHR110008) is a compound with antitumor activity that has specific pharmacokinetic properties in rats and is rapidly distributed to normal tissues. The kidney is the major excretion organ, and its plasma protein binding capacity is nearly linearly related to concentration.
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- HY-123011
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SHR3824
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SGLT
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Metabolic Disease
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Henagliflozin (SHR3824) is a potent selective sodium-glucose co-transporter 2 (SGLT2) inhibitor with the IC50 values of 2.38 and 4324 nM for human SGLT2 and SGLT1, respectively. Henagliflozin can be used in diabetes research .
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- HY-136625
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Others
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Neurological Disease
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LY134046 is an inhibitor of norepinephrine N-methyltransferase (NMT). Its cardiovascular activity was studied in anesthetized spontaneously hypertensive rats (SHR). Acute intraperitoneal injection of 10 and 20 mg/kg of LY134046 caused minimal cardiovascular changes, while 40 mg/kg resulted in a sustained decrease in mean arterial blood pressure and heart rate. This hypotension and bradycardia occurred rapidly and occurred when brain NMT activity was significantly inhibited. However, norepinephrine concentrations in rat brains were not significantly reduced at the time when LY134046-induced blood pressure and heart rate effects were maximal. The acute cardiovascular activity of LY134046 was not significantly affected by pretreatment of SHR with phentolamine, propranolol, or atropine, and LY134046 reduced heart rate in suspended SHR. In addition, acute or chronic administration of LY134046 did not antagonize the vasoconstrictor responses induced by sympathetic nerve stimulation or exogenous norepinephrine. These observations suggest that LY134046 does not interact with adrenergic or cholinergic receptors and that its hypotensive and bradycardic effects do not require neurogenic tension. Chronic intraperitoneal administration of LY134046 (40 mg/kg/day) resulted in a sustained and significant inhibition of hypothalamic and brainstem NMT activity, leading to central norepinephrine depletion. During chronic treatment, norepinephrine and dopamine concentrations increased in the brainstem and hypothalamus of SHR. Despite chronic inhibition of central NMT and norepinephrine depletion, cardiovascular parameters in SHR treated groups were not significantly different from those in saline-injected controls. Chronic treatment with LY134046 did not result in tolerance to its central biochemical effects or acute cardiovascular activity. The present study does not support the idea that norepinephrine-producing neurons are involved in the central regulation of cardiovascular function, because the hypotension and bradycardia induced by acute administration of LY134046 occurred before a significant decrease in hypothalamic norepinephrine concentrations, whereas chronic inhibition of central NMT and depletion of norepinephrine resulted in minimal changes in baseline cardiovascular parameters.
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- HY-107398
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Others
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Cardiovascular Disease
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1-(2,3-Dichlorophenyl)ethanamine hydrochloride is a phenylethanolamine N-methyltransferase (PNMT) inhibitor. 1-(2,3-Dichlorophenyl)ethanamine hydrochloride effectively reduces blood pressure of spontaneously hypertensive. 1-(2,3-Dichlorophenyl)ethanamine hydrochloride can be used for the research of blood pressure .
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- HY-P4296
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Amino Acid Derivatives
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Others
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H-Gly-Sar-Sar-OH is an orally active tripeptide. H-Gly-Sar-Sar-OH is transported through PepT1 within Caco-2 cells. H-Gly Sar Sar OH has potential applications in material transportation .
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- HY-108713
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SHR1020
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VEGFR
PDGFR
Apoptosis
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Cancer
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Famitinib (SHR1020), an orally active multi-targeted kinase inhibitor, inhibits the activity of c-kit, VEGFR-2 and PDGFRβ with IC50 values of 2.3 nM, 4.7 nM and 6.6 nM, respectively . Famitinib exerts powerful antitumor activity in human gastric cancer cells and xenografts. Famitinib triggers apoptosis .
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- HY-A0117
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Temocapril diacid; Temocaprilate; RS 5139
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Angiotensin-converting Enzyme (ACE)
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Cardiovascular Disease
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Temocaprilat (Temocapril diacid) is an inhibitor of angiotensin-converting enzyme (ACE). Temocaprilat alleviates the inhibitory effect of high glucose on the proliferation of aortic endothelial cells. Temocaprilat has potential applications in hypertension and vascular inflammation .
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- HY-116680
-
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5-HT Receptor
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Cardiovascular Disease
Neurological Disease
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LY53857 is a potent antagonist of vasoconstriction and serotonin-mediated 5-HT2 receptors. LY53857 did not reduce mean arterial blood pressure in spontaneously hypertensive rats (SHR) at doses that blocked the depressor response to serotonin and blocked central serotonin receptors. In addition, LY53857 was able to enhance neurotransmitter release in rat vas deferens and guinea pig ileal nerves .
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- HY-108713A
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SHR1020 malate
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VEGFR
PDGFR
Apoptosis
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Cancer
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Famitinib (SHR1020) malate, an orally active multi-targeted kinase inhibitor, inhibits the activity of c-kit, VEGFR-2 and PDGFRβ with IC50 values of 2.3 nM, 4.7 nM and 6.6 nM, respectively. Famitinib malate induces cell apoptosis. Famitinib malate exerts powerful antitumor activity in human gastric cancer cells and xenografts, it can be used for the research of cancer .
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- HY-108713R
-
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VEGFR
PDGFR
Apoptosis
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Cancer
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Famitinib (Standard) is the analytical standard of Famitinib. This product is intended for research and analytical applications. Famitinib (SHR1020), an orally active multi-targeted kinase inhibitor, inhibits the activity of c-kit, VEGFR-2 and PDGFRβ with IC50 values of 2.3 nM, 4.7 nM and 6.6 nM, respectively . Famitinib exerts powerful antitumor activity in human gastric cancer cells and xenografts. Famitinib triggers apoptosis .
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- HY-112724
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SHR0302
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JAK
Apoptosis
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Inflammation/Immunology
Cancer
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Ivarmacitinib (SHR0302) is a potent and orally active all members of the JAK family inhibitor, particularly JAK1. The selectivity of Ivarmacitinib for JAK1 is >10-fold for JAK2, 77-fold for JAK3, 420-fold for Tyk2. Ivarmacitinib inhibits JAK1-STAT3 phosphorylation and induces the apoptosis of hepatic stellate cells. Ivarmacitinib has anti-proliferative and anti-inflammatory effects .
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- HY-106720
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YM 09538
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Adrenergic Receptor
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Cardiovascular Disease
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Amosulalol (YM 09538) is an orally active and dual inhibitor of α1/β1-Adrenergic Receptor. Amosulalol exhibits antihypertensive activity via α1-Adrenergic Receptor inhibition. Amosulalol decreases reflexogenic increases in heart rate and plasma renin activity (PRA) via β1-Adrenergic Receptor inhibition in spontaneously hypertensive rats (SHR) .
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- HY-112724A
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SHR0302 sulfate
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JAK
Apoptosis
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Inflammation/Immunology
Cancer
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Ivarmacitinib (SHR0302) sulfate is a potent and orally active all members of the JAK family inhibitor, particularly JAK1. The selectivity of Ivarmacitinib for JAK1 is >10-fold for JAK2, 77-fold for JAK3, 420-fold for Tyk2. Ivarmacitinib inhibits JAK1-STAT3 phosphorylation and induces the apoptosis of hepatic stellate cells. Ivarmacitinib has anti-proliferative and anti-inflammatory effects .
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- HY-106720A
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YM 09538 hydrochloride
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Adrenergic Receptor
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Cardiovascular Disease
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Amosulalol (YM 09538) hydrochloride is an orally active and dual inhibitor of α1/β1-Adrenergic Receptor. Amosulalol hydrochloride exhibits antihypertensive activity via α1-Adrenergic Receptor inhibition. Amosulalol hydrochloride decreases reflexogenic increases in heart rate and plasma renin activity (PRA) via β1-Adrenergic Receptor inhibition in spontaneously hypertensive rats (SHR) .
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-
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- HY-164762
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SHR-A1811
|
Antibody-Drug Conjugates (ADCs)
EGFR
|
Cancer
|
Trastuzumab rezetecan (SHR-A1811) is a HER2-targeting antibody-drug conjugate (ADC). Trastuzumab rezetecan is composed of a humanized anti-HER2 antibody (HY-P9907), a cleavable linker MC-Gly-Gly-Phe-Gly (HY-44246), and a topoisomerase I inhibitor payload Rezetecán (HY-147408). Trastuzumab rezetecan can be used for research in HER2-positive breast cancer .
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-
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- HY-N9113
-
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Others
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Cardiovascular Disease
|
1,3,5,6-Tetrahydroxyxanthone is a natural xanthone that can be isolated from Garcinia achachairu Rusby (Clusiaceae) branches. 1,3,5,6-Tetrahydroxyxanthone induces diuresis and saluresis in normotensive and hypertensive rats .
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- HY-114778
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SHR3162; Fuzuloparib
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PARP
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Cancer
|
Fluzoparib (SHR3162) is a potent and orally active PARP1 inhibitor (IC50=1.46±0.72 nM, a cell-free enzymatic assay) with superior antitumor activity. Fluzoparib selectively inhibits the proliferation of homologous recombination repair (HR)-deficient cells, and sensitizes both HR-deficient and HR-proficient cells to cytotoxic agents. Fluzoparib exhibits good pharmacokinetic properties in vivo and can be used for BRCA1/2-mutant relapsed ovarian cancer research .
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-
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- HY-153369
-
|
Guanylate Cyclase
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Cardiovascular Disease
Neurological Disease
|
BAY-747 is an orally active and brain-penetrant stimulator of soluble guanylate cyclase (sGC). BAY-747 reverses L-NAME induced memory impairments and enhances cognition of rats in the object location task (OLT). BAY-747 also decreases blood pressure in both conscious normotensive and spontaneously hypertensive rats (SHR). BAY-747 improves function of the skeletal muscle associated with Duchenne muscular dystrophy (DMD) in mdx/mTRG2 mice model .
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-
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- HY-139792
-
SHR117887
|
Others
|
Metabolic Disease
|
Besigliptin tosylate (SHR117887) is a DPP-4 inhibitor with activity to improve metabolic control and β-cell function. Besigliptin tosylate can effectively reduce serum DPP-4 activity and improve oral glucose tolerance. Besigliptin tosylate significantly reduces fasting blood glucose levels and improves lipid profiles in a diabetic mouse model. The effect of besigliptin tosylate is comparable to that of the known compound vildagliptin (HY-14291) at the same concentration. Besigliptin tosylate increases insulin staining of pancreatic islet cells in chronic administration, indicating improved β-cell function .
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-
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- HY-B0612
-
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Calcium Channel
Apoptosis
Reactive Oxygen Species
p38 MAPK
NF-κB
|
Cardiovascular Disease
Neurological Disease
|
Lercanidipine is a third-generation, lipophilic, brain-penetrant, vascular-selective and orally active dihydropyridine-calcium channel blocker with a pIC50 of 7.74 (converts from μM). Lercanidipine has long lasting antihypertensive action as well as reno- and neuro-protective effect. Lercanidipine also shows anti-oxidant, anti-inflammatory and anti-apoptotic properties. Lercanidipine can be used in cardiovascular and neurological research .
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-
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- HY-B0612A
-
|
Calcium Channel
Apoptosis
Reactive Oxygen Species
p38 MAPK
NF-κB
|
Cardiovascular Disease
Neurological Disease
|
Lercanidipine is a third-generation, lipophilic, brain-penetrant, vascular-selective and orally active dihydropyridine-calcium channel blocker with a pIC50 of 7.74 (converts from μM). Lercanidipine has long lasting antihypertensive action as well as reno- and neuro-protective effect. Lercanidipine also shows anti-oxidant, anti-inflammatory and anti-apoptotic properties. Lercanidipine can be used in cardiovascular and neurological research .
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-
-
- HY-B0612AR
-
|
Calcium Channel
Apoptosis
Reactive Oxygen Species
p38 MAPK
NF-κB
|
Cardiovascular Disease
Neurological Disease
|
Lercanidipine (hydrochloride) (Standard) is the analytical standard of Lercanidipine (hydrochloride). This product is intended for research and analytical applications. Lercanidipine is a third-generation, lipophilic, brain-penetrant, vascular-selective and orally active dihydropyridine-calcium channel blocker with a pIC50 of 7.74 (converts from μM). Lercanidipine has long lasting antihypertensive action as well as reno- and neuro-protective effect. Lercanidipine also shows anti-oxidant, anti-inflammatory and anti-apoptotic properties. Lercanidipine can be used in cardiovascular and neurological research .
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-
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- HY-103247
-
|
Angiotensin Receptor
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Cardiovascular Disease
|
EMD 66684 is an antagonist of Angiotensin II Type 1 (AT1) receptor. EMD 66684 shows potent binding affinities for the AT1 subtype Ang II receptor with an IC50 value of 0.7 nM. EMD 66684 also serves as an antiischemic cytoprotectant - .
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-
Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P10318
-
|
GLP Receptor
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Endocrinology
|
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 .
|
-
- HY-P4296
-
|
Amino Acid Derivatives
|
Others
|
H-Gly-Sar-Sar-OH is an orally active tripeptide. H-Gly-Sar-Sar-OH is transported through PepT1 within Caco-2 cells. H-Gly Sar Sar OH has potential applications in material transportation .
|
Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P99944
-
Retlirafusp alfa
|
PD-1/PD-L1
TGF-β Receptor
|
Cancer
|
SHR-1701 (Retlirafusp alfa) is a bifunctional fusion protein targeting PD-L1 and TGF-β for cancer research .
|
-
- HY-P99422
-
SHR-1316
|
PD-1/PD-L1
Apoptosis
|
Cancer
|
Adebrelimab (SHR-1316) is a humanized IgG4 monoclonal PD-L1 (PD-1/PD-L1) antibody. Adebrelimab has promising antitumor activity in solid tumors including extensive-stage small-cell lung cancer (SCLC) .
|
-
- HY-P99822
-
SHR-1209
|
PCSK9
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Metabolic Disease
|
Recaticimab (SHR-1209) is a humanized monoclonal antibody that inhibits PCSK9. Recaticimab can bind to PCSK9 and mediate its degradation, increasing the level of low-density lipoprotein (LDL) receptors on the surface of liver cells, reducing the level of LDL in plasma, thereby lowering blood lipids. Recaticimab can be used for the study of hypercholesterolemia .
|
-
- HY-P9971
-
SHR-1210
|
PD-1/PD-L1
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Cancer
|
Camrelizumab (SHR-1210) is a potent humanied high-affinity IgG4-κ monoclonal antibody (mAb) to PD-1. Camrelizumab binds PD-1 at a high affinity of 3 nM and inhibits the binding interaction of PD-1 and PD-L1 with an IC50 of 0.70 nM. Camrelizumab acts as anti-PD-1/PD-L1 agent and can be used for cancer research, including NSCLC, ESCC, Hodgkin lymphoma, and advanced HCC et,al .
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Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
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