Stampidine

斯坦皮丁

Stampidine

S649252-5mg

5mg

≥99%

-20°C储存

超低温冰袋运输

Stampidine is a nucleoside reverse transcriptase inhibitor (NRTI) with potent and broad-spectrum anti-HIV activity. Stampidine inhibits the laboratory HIV-1 strain HTLV IIIB (B-envelope subtype) and primary clinical isolates with IC 50 s of 1 nM and 2 nM, respectively. Stampidine also inhibits NRTI-resistant primary clinical isolates and NNRTI-resistant clinical isolates with IC 50 s of 8.7 nM and 11.2 nM, respectively In Vitro Stampidine (7.8-1,000 μM; 24 hours) is not cytotoxic to genital tract epithelial cells. Stampidine has no effect on sperm motility in cervical mucus. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo Stampidine (50-100 mg/kg; p.o.) exhibits potent antiretroviral activity in chronically feline immunodeficiency virus (FIV)-infected cats. Stampidine (100 mg/kg; p.o.) shows the average plasma C max , AUC, half-life (t 1/2 ), and mean residence time (MRT) values of 15.4 µM, 23.1 µM•h, 108.6 min and 119.4 min, respectively, in dogs. Stampidine does not cause anemia, thrombocytopenia, neutropenia, or lymphopenia suggestive of hematologic toxicity, elevations of BUN or creatinine or electrolyte disturbances suggestive of renal toxicity or metabolic abnormalities, elevations of ALT, AST, Alk in adult beagle dogs. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: SPF male or female domestic cats (2.9- 6.2 kg), with chronically FIV-infectedDosage: 50 mg/kg, 100 mg/kg Administration: Oral administration (oral bolus dose) Result: Exhibited potent antiretroviral activity. Animal Model: Male beagle dogs (10-12 kg)Dosage: 100 mg/kg (Pharmacokinetic Analysis) Administration: Oral administration Result: The estimated average plasma C max and AUC values were 15.4 µM and 23.1 µM·h, respectively. The average elimination half-life (t 1/2 ) and mean residence time (MRT) were 108.6 min and 119.4 min, respectively. Form:Solid IC50& Target:IC50: 1 nM (HTLV IIIB ), 2 nM (primary clinical isolates), 8.7 nM (NRTI-resistant primary clinical isolates), 11.2 nM (NRTI-resistant primary clinical isolates)

Stampidine是一种核苷类逆转录酶抑制剂（NRTI），具有强效、广谱的抗艾滋病毒活性。斯坦普定对实验室 HIV-1 株 HTLV IIIB（B-包膜亚型）和原发性临床分离株具有抑制作用，IC 50 s 为 1 nM 和 2 nM、

217178-62-6

C20H23BrN3O8P

544.29 g/mol

469782

CC1=CN(C(=O)NC1=O)[C@H]2C=C[C@H](O2)COP(=O)(N[C@H](C)C(=O)OC)OC3=CC=C(C=C3)Br

CC1=CN(C(=O)NC1=O)[C@H]2C=C[C@H](O2)COP(=O)(N[C@H](C)C(=O)OC)OC3=CC=C(C=C3)Br

469782

DMSO : 100 mg/mL (183.73 mM; Need ultrasonic)

2

9

10

543.041 Da

543.041 Da

133.000 Ų

33

0

873.000

0

1

1.700