HIF-PHD-IN-1
HIF-PHD-IN-1 是一种具有口服活性的缺氧诱导因子脯氨酰羟化酶结构域 (HIF-PHD) 的抑制剂，抑制 hHIF-PHD2 的 IC50 值为 54 nM。HIF-PHD-IN-1 是有希望的肾性贫血研究药物。
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包装价格促销价数量
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10mg￥8850.007080.00- +
- 货号: ajcf17594
- CAS: 1567657-46-8
- 别名:
- 分子式: C17H12Cl2N6O3
- 分子量: 419.22
- 纯度: ＞98%
- 溶解度:
- 储存: 4°C, away from moisture and light
- 库存: 现货
Background
IC50: 54 nM (hHIF-PHD2)[1]
HIF-PHD-IN-1 is an orally active inhibitor of hypoxia-inducible factor prolyl hydroxylase domain (HIF-PHD), with an IC50 of 54 nM for hHIF-PHD2. HIF-PHD-IN-1 is promising therapeutic agents for renal anemia[1].
HIF-PHD-IN-1 (compound 19) (0.5-2 mg/kg; p. o. once daily for 4 weeks) improves hemoglobin levels in anemic rats[1].
HIF-PHD-IN-1 (10 mg/kg; single p.o.) increases serum erythropoietin (EPO) concentration at 8 h after administration in SD rats[1].
HIF-PHD-IN-1 (1 mg/kg; p.o.) shows good bioavailability (F=77%) in male SD rats[1].
| Animal Model: | Male SD Rats excising ?ve-sixths of their kidneys[1] |
| Dosage: | 0.5, 1, 2 mg/kg |
| Administration: | P.o. once daily for 4 weeks |
| Result: | Improved blood hemoglobin levels starting at weeks 2 and 1 in the groups receiving 1 and 2 (mg/kg)/day, respectively. |
| Animal Model: | Male SD Rats[1] |
| Dosage: | 1 mg/kg (Pharmacokinetic Analysis) |
| Administration: | Single p.o. or i.v. |
| Result: | Cmax=1839 ng/mL (p.o.); Cmax=12357ng/mL (i.v.); F=77%. |
[1]. Goi T, et, al. Pyrazolo[4,3- d]pyrimidine Derivatives as a Novel Hypoxia-Inducible Factor Prolyl Hydroxylase Domain Inhibitor for the Treatment of Anemia. ACS Med Chem Lett. 2020 Jun 4; 11(7): 1416-1420.
