Acetic acid, 2-[4-[5-(3-chlorophenoxy)oxazolo[5,4-d]pyrimidin-2-yl]-2,6-dimethylphenoxy]-
- CAS No.
- 1315311-14-8
- Chemical Name:
- Acetic acid, 2-[4-[5-(3-chlorophenoxy)oxazolo[5,4-d]pyrimidin-2-yl]-2,6-dimethylphenoxy]-
- Synonyms
- SAR247799;S1P1 agonist 3;{4-[5-(3-chlorophenoxy)oxazolo[5,4-d]pyrimidin-2-yl]-2,6-dimethylphenoxy}acetic acid;Acetic acid, 2-[4-[5-(3-chlorophenoxy)oxazolo[5,4-d]pyrimidin-2-yl]-2,6-dimethylphenoxy]-
- CBNumber:
- CB29323841
- Molecular Formula:
- C21H16ClN3O5
- Molecular Weight:
- 425.82
- MDL Number:
- MOL File:
- 1315311-14-8.mol
- MSDS File:
- SDS
- TDS File:
- TDS
Acetic acid, 2-[4-[5-(3-chlorophenoxy)oxazolo[5,4-d]pyrimidin-2-yl]-2,6-dimethylphenoxy]- price
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| ChemScene | CS-0368765 | SAR247799 99.38% | 1315311-14-8 | 5mg | $520 | 2026-06-04 | Buy |
| ChemScene | CS-0368765 | SAR247799 99.38% | 1315311-14-8 | 10mg | $867 | 2026-06-04 | Buy |
| ChemScene | CS-0368765 | SAR247799 99.38% | 1315311-14-8 | 25mg | $1787 | 2026-06-04 | Buy |
| ChemScene | CS-0368765 | SAR247799 99.38% | 1315311-14-8 | 50mg | $2817 | 2026-06-04 | Buy |
| ChemScene | CS-0368765 | SAR247799 99.38% | 1315311-14-8 | 100mg | $4333 | 2026-06-04 | Buy |
Acetic acid, 2-[4-[5-(3-chlorophenoxy)oxazolo[5,4-d]pyrimidin-2-yl]-2,6-dimethylphenoxy]- Chemical Properties, Uses, Production
Description
SAR247799 is a novel G-protein-biased sphingosine-1 phosphate receptor-1 (S1P1) agonist.
Uses
SAR247799 (S1P1 agonist 3) is an oral activity, selective G-protein-biased sphingosine-1 phosphate receptor-1 (S1P1 ) agonist, with EC50s rang from 12.6 to 493 nM in S1P1-overexpressing cells and HUVECs. SAR247799 can be used for the research of endothelial protection, including type-2 diabetes, metabolic syndrome[1][2][3][4].
in vivo
SAR247799 (1 and 3 mg/kg; p.o.; 1 h before renal occlusion) dose dependently reduces the severity of ischemia/reperfusion (I/R)–induced acute kidney injury[1].
SAR247799 (0.3, 1, 3 mg/kg; i.v.) dose dependently increases the coronary conductance ratio in pig model of coronary endothelial dysfunction[1].
SAR247799 (30-min intravenous administration; 8- to 10-week-old farm pig) exposure (Cmax and AUC) increases with dose in pigs. Pharmacokinetic parameters [1]:
| Dose (mg/kg) | N | Cmax (g/mL) | Tmax (h) | Tlast (h) | AUC0-last (g.h/mL) | Cl (L/h/kg) | Vss (L/kg) | T1/2z (h) |
| 1 | 4 | 2.08 (8) | 0.5 [0.5] | [8-48] | 11.8 (46) | 0.113 (75) | 0.516 (11) | 5.62 (57) |
| 3 | 7 | 8.10 (12) | 0.5 [0.5] | [24-72] | 42.2 (23) | 0.0754 (30) | 0.446 (16) | 6.21 (28) |
| 10 | 3 | 36.7 (5) | 0.5 [0.5-0.75] | 72 | 294 (13) | 0.0343 (13) | 0.338 (7) | 7.73 (8) |
| 30 | 6 | 112 (27) | 0.5 [0.5- 1.0] | [48-72] | 908 (16) | 0.0338 (18) | 0.294 (11) | 7.35 (11) |
| Animal Model: | Acute kidney injury rats (12 to 15-week-old Fischer rats)[1] |
| Dosage: | 1 and 3 mg/kg |
| Administration: | P.o.; administered 1 hour before renal occlusion. |
| Result: | Inhibited the increase in serum creatinine (89 and 96% at 1 and 3 mg/kg) and urea (61 and 85% at 1 and 3 mg/kg). Protected renal proximal tubules against necrosis and blunted the development of interstitial hemorrhage. |
| Animal Model: | Acute kidney injury rats (8- to 12-week-old Fischer rats)[1] |
| Dosage: | 3 mg/kg |
| Administration: | P.o.; twice a day for 7 days and twice a day for 7 day |
| Result: | Showed a dosedependent trend for reducing macrophage. |
IC 50
S1PR1: 12.6-493 nM (EC50)
References
[1] Poirier B, et al. A G protein-biased S1P1 agonist, SAR247799, protects endothelial cells without affecting lymphocyte numbers. Sci Signal. 2020 Jun 2;13(634):eaax8050. DOI:10.1126/scisignal.aax8050
[2] Evaristi MF, et al. A G-protein-biased S1P1 agonist, SAR247799, improved LVH and diastolic function in a rat model of metabolic syndrome. PLoS One. 2022 Jan 14;17(1):e0257929. DOI:10.1371/journal.pone.0257929
[3] Bergougnan L, et al. Endothelial-protective effects of a G-protein-biased sphingosine-1 phosphate receptor-1 agonist, SAR247799, in type-2 diabetes rats and a randomized placebo-controlled patient trial. Br J Clin Pharmacol. 2021 May;87(5):2303-2320. DOI:10.1111/bcp.14632
[4] Bergougnan L, et al. First-in-human study of the safety, tolerability, pharmacokinetics and pharmacodynamics of single and multiple oral doses of SAR247799, a selective G-protein-biased sphingosine-1 phosphate receptor-1 agonist for endothelial protection DOI:10.1111/bcp.14422
Acetic acid, 2-[4-[5-(3-chlorophenoxy)oxazolo[5,4-d]pyrimidin-2-yl]-2,6-dimethylphenoxy]- Preparation Products And Raw materials
Raw materials
Preparation Products
Acetic acid, 2-[4-[5-(3-chlorophenoxy)oxazolo[5,4-d]pyrimidin-2-yl]-2,6-dimethylphenoxy]- Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Shanghai Merlot Chemical Co., LTD | 15821661757 | 226174156@qq.com | China | 476 | 58 |
| Shanghai Yifei Biotechnology Co. , Ltd. | 021-65675885 18964387627 | customer_service@efebio.com | China | 11963 | 58 |
| RD International Technology Co., Limited | 18024082417 | market@ubiochem.com | China | 9831 | 58 |
| TargetMol Chemicals Inc. | 15002134094 | marketing@targetmol.cn | China | 29873 | 58 |
| Shanghai Amole Biotechnology Co., Ltd. | 13370042665 18916960931 | 2596183085@qq.com | China | 17234 | 58 |
| Hebei Yaocheng Pharmaceutical Technology Co. Ltd | 19903117580 19903117510 | yc-eliu@yaochengph.com | China | 9949 | 58 |
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