Search results for: 'sar 100842'
Catalog No.
Product Name
Application
Product Information
Product Citation
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lysophaphatidic acid 1 (LPA1/Edg-2) receptor inhibitor
SAR-100842 is a lysophaphatidic acid 1 (LPA1/Edg-2) receptor inhibitor. -
Aurora Kinase inhibitor
SAR156497 is an exquisitely selective Aurora A, B, and C inhibitor with in vitro and in vivo efficacy with IC50 = 0.5 nM (Aurora A), 1 nM (Aurora B / incenp), 3 nM (Aurora C / incenp) respectively SAR156497 combines high in vitro potency with satisfactory metabolic stability and limited CYP3A4 and PDE3 inhibition. -
ROCK inhibitor
SAR407899 is a potent and selective Rho kinase inhibitor with promising antihypertensive activity. -
PIK3C3/Vps34 inhibitor
SAR405 R enantiomer is the less active enantiomer of SAR405. SAR405 is a PIK3C3/Vps34 inhibitor. -
TRPC6 inhibitor
SAR7334 is a novel, highly potent and bioavailable inhibitor of TRPC6 channels that opens new opportunities for the investigation of TRPC channel function in vivo. SAR7334 inhibited TRPC6, TRPC3 and TRPC7-mediated Ca(2+) influx into cells with IC50 s of 9.5, 282 and 226 nM, whereas TRPC4 and TRPC5-mediated Ca(2+) entry was not affected. -
Estrogen receptor degrader
SAR439859 is an orally available, nonsteroidal selective estrogen receptor degrader/downregulator (SERD). -
PI3K/mTOR dual inhibitor
SAR245409 is a PI3K/mTOR dual kinase inhibitor XL765 is an orally bioavailable small molecule targeting the phosphatidylinositol 3 kinase (PI3K) and mammalian target of rapamycin (mTOR) kinases in the PI3K/mTOR signaling pathway, with potential antineoplastic activity. -
O-GlcNAcase inhibitor
Streptozotocin (Streptozocin, Zanosar, STZ)is used in medical research to produce an animal model for Type 1 diabetes, which directly inhibist the O-GlcNAcase activity of the enzyme NCOAT in vitro.- Zhen Liang, .et al. , Nat Metab, 2023, Jan;5(1):29-40 PMID: 36624157
- Alemayehu Toma, .et al. , J Exp Pharmacol, 2022, 14: 309-316 PMID: 36317069
- Andressa Braga, .et al. , Braz J Pharm Sci, 2022, 58: e19674
- Yuanyuan Du, .et al. , Nat Med, 2022, Feb;28(2):272-282 PMID: 35115708
- Karemah A. Alatawi, .et al. , Saudi Journal of Biological Sciences, 2021, 25 June
- D.H. Mhya, .et al. , Asian J Exp Biol Sci, 2019, 12 (2): 164-172
- Stanley I. R. Okoduwa, .et al. , J Diabetol, 2017, 8(3): 74-85
- Stanley I. R. Okoduwa, .et al. , Medicines (Basel), 2017, Dec; 4(4): 73 PMID: 29019956
- Stanley I. R. Okoduwa, .et al. , PLoS One, 2017, 12(1): e0170971 PMID: 28129400
- Stanley I. R. Okoduwa, .et al. , World J Diabetes, 2016, Dec 15; 7(20): 605-614 PMID: 28031778
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non-peptide angiotensin II receptor antagonist
Fimasartan is a non-peptide angiotensin II receptor antagonist (ARB) used for the treatment of hypertension and heart failure. Through oral administration, fimasartan blocks angiotensin II receptor type 1 (AT1 receptors), reducing pro-hypertensive actions of angiotensin II, such as systemic vasoconstriction and water retention by the kidneys. -
angiotensin II receptor type 1 antagonist
Azilsartan medoxomil monopotassium is an orally administered angiotensin II receptor type 1 antagonist with IC50 of 0.62 nM, which used in the treatment of adults with essential hypertension. -
CHK1 inhibitor
SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC50 of 13.3 nM for human CHK1. -
Src/Abl inhibitor
Saracatinib (AZD0530) is a highly selective, orally available, dual-specific Src/Abl kinase inhibitor with IC50 of 2.7 and 30 nM for c-Src and Abl kinase, respectively.- Andromachi Lambrianidou, .et al. , Cell Signal, 2021, Apr;80:109912 PMID: 33388443
- Chisato Naito, .et al. , Atherosclerosis, 2016, Mar;246:344-51 PMID: 26828753
- Kenta Maruyama, .et al. , J Biol Chem, 2015, Apr 10; 290(15): 9377-9386 PMID: 25691576
- Amanda L Jackson, .et al. , Expert Opin Emerg Drugs, 2015, Jun;20(2):331-46 PMID: 26001052
- Candesartan is an angiotensin II receptor antagonist used mainly for the treatment of hypertension.
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AT1 antagonist
Irbesartan is an angiotensin II receptor antagonist used mainly for the treatment of hypertension. - Olmesartan is an angiotensin II receptor antagonist indicated for the treatment of hypertension. It may be used alone or in combination with other antihypertensive agents.
- Takashi Azuma, .et al. , SEP PURIF TECHNOL, 2019, Apr; 212: 483-489
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Angiotensin II receptor antagonist
Tasosartan is an angiotensin II receptor antagonist. -
AT1 receptor antagonist
Eprosartan is an angiotensin II receptor antagonist used for the treatment of high blood pressure. - Olmesartan medoxomil is an angiotensin II receptor antagonist used to treat high blood pressure. Olmesartan works by blocking the binding of angiotensin II to the AT1 receptors in vascular muscle. By blocking the binding rather than the synthesis of angiotensin II, olmesartan inhibits the negative regulatory feedback on renin secretion.
- Takashi Azuma, .et al. , SEP PURIF TECHNOL, 2019, Apr; 212: 483-489
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Topoisomerase inhibitor
Sarafloxacin hydrochloride is a fluoroquinolone antibacterial agent. Inhibits bacterial DNA gyrase (topoisomerase). -
AT1 Receptor Blocker
Azilsartan (TAK-536) is an angiotensin II receptor antagonist used in the treatment of hypertension. - Sarsasapogenin is a steroidal sapogenin, that is the aglycosidic portion of a plant saponin. Sarsasapogenin and its C-25 epimer smilagenin lowered blood sugar and reversed diabetic weight gain in experiments within mice with a mutant diabetes gene (db).
- Eprosartan (mesylate) is a competitive AT1 receptor antagonist with IC50 values ranging from 1.4 ?€? 3.9 nM and an elimination half-life of five to seven hours.
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angiotensin II receptor type 1 antagonist
Azilsartan medoxomil is an orally administered angiotensin II receptor type 1 antagonist with IC50 of 0.62 nM, which used in the treatment of adults with essential hypertension. -
polyamine synthesis inhibitor
Sardomozide is a second-generation polyamine synthesis inhibitor, which inhibits the activity of the polyamine biosynthetic enzyme S-adenosylmethionine decarboxylase (SAMDC). -
5-HT2 antagonist
Sarpogrelate hydrochloride (MCI-9042), a selective 5-HT2 antagonist, has been widely used as an anti-platelet agent for the treatment of PAD. -
aldose reductase inhibitor
Risarestat (CT-112), an aldose reductase inhibitor, is developed for the treatment of diabetic complications -
angiotensin II receptor antagonist
Losartan D4 Carboxylic Acid is the deuterium labeled Losartan(EXP-3174), which is an angiotensin II receptor antagonist. -
angiotensin II type 1 receptor antagonist
Azilsartan D5 is the deuterium labeled Azilsartan(TAK-536), which is a specific and potent angiotensin II type 1 receptor antagonist. -
ALK/MET inhibitor
Ensartinib hydrochloride (X-396 hydrochloride) is a potent and dual ALK/MET inhibitor with IC50s of <0.4 nM and 0.74 nM, respectively. -
benzodiazepine receptor antagonist
Sarmazenil is a benzodiazepine receptor antagonist. -
PPAR agonist
Saroglitazar is a novel peroxisome proliferator-activated receptor (PPAR) agonist with predominant PPARα and moderate PPARγ activity with EC50 values of 0.65 pM and 3 nM in HepG2 cells, respectively. -
ACC inhibitor
Olumacostat glasaretil is a small molecule inhibitor of acetyl coenzyme A carboxylase (ACC). -
angiotensin II receptor antagonist
Pratosartan is a selective angiotensin II receptor antagonist. -
ALK/MET inhibitor
Ensartinib (X-396) is a potent and dual ALK/MET inhibitor with IC50s of <0.4 nM and 0.74 nM, respectively.
