ALS-8176 纯度:>98.0% 50mg

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Qiagen 凯杰 Biosharp Omega

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首页酶、辅酶及抑制剂MCE>

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ALS-8176 纯度:>98.0% 50mg

市场价：: 15000.00

促销价：: ¥15000.00

货号：HY-12983A

品牌：MCE

配送至：

北京朝阳

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支 (预计4-5工作日到货(以MCE官网货期为准))

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周一至周五：9:00-18:00

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商品介绍
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ALS-8176是呼吸道合胞病毒（RSV）聚合酶的抑制剂。

Description

ALS-8176 an inhibitor of the respiratory syncytial virus (RSV) polymerase.

In Vitro

ALS-008176 is an orally bioavailable prodrug of the novel RSV replication inhibitor ALS-008112, a cytidine nucleoside analogue^[1].

In Vivo

ALS-8176 demonstrates excellent anti-RSV efficacy and safety in a phase 2 clinical RSV challenge study. It exhibits good oral bioavailability and a high level of 2c-TP in vivo. ALS-8176 has excellent stability profiles in formulations (>24 h storage stability in 0.5% methylcellulose aqueous formulation at rt) and simulats gastric and intestinal fluids (half-life >2 h). Its solubility is adequate to support oral administration in solutions with relatively low percentage of organic solvent and in aqueous suspensions. High levels of NMP and NTP are obtained following oral administration of ALS-8176 to monkeys^[2]. In an adult human challenge study, ALS-8176 has shown efficacy against RSV infection^[1].

Solvent & Solubility

In Vitro:

DMSO : ≥ 50 mg/mL (115.24 mM)

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.3049 mL	11.5245 mL	23.0489 mL
5 mM	0.4610 mL	2.3049 mL	4.6098 mL
10 mM	0.2305 mL	1.1524 mL	2.3049 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO 90% corn oil

Solubility: ≥ 2.5 mg/mL (5.76 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.5 mg/mL (5.76 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (5.76 mM); Clear solution

References

[1]. DeVincenzo JP, et al. Activity of Oral ALS-008176 in a Respiratory Syncytial Virus Challenge Study. N Engl J Med. 2015 Nov 19;373(21):2048-58.

[2]. Wang G, et al. Discovery of 4'-chloromethyl-2'-deoxy-3',5'-di-O-isobutyryl-2'-fluorocytidine (ALS-8176), a first-in-class RSV polymerase inhibitor for treatment of human respiratory syncytial virus infection. J Med Chem. 2015 Feb 26;58(4):1862-78.

Kinase Assay ^[2]	Cell fractionation and extraction of RSV RNP complex is performed. Nucleoside triphosphate (NTP) concentrations are: 0.1 μM CTP and 1 μM ATP, 2 μM UTP, and 500 μM GTP. The radioactive tracer is either 10 μCi [α-³³P]rCTP or 15 μCi MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[2]	Rats: ALS-8176 are formulated as solutions in PEG400-based vehicles. Pharmacokinetic studies are conducted at 5 mg/kg and for oral PK studies the prodrugs are administered at 5 mg/kg parent nucleoside equivalent doses. Blood samples are typically collected at various time points up to 24 h post dose for rat^[2]. Monkeys: ALS-8176 are formulated as solutions in PEG400-based vehicles. Pharmacokinetic studies are conducted at 5 mg/kg and for oral PK studies the prodrugs are administered at 5 mg/kg parent nucleoside equivalent doses. Blood samples are typically collected at various time points up to 12 h post dose for Monkeys^[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. DeVincenzo JP, et al. Activity of Oral ALS-008176 in a Respiratory Syncytial Virus Challenge Study. N Engl J Med. 2015 Nov 19;373(21):2048-58. [2]. Wang G, et al. Discovery of 4'-chloromethyl-2'-deoxy-3',5'-di-O-isobutyryl-2'-fluorocytidine (ALS-8176), a first-in-class RSV polymerase inhibitor for treatment of human respiratory syncytial virus infection. J Med Chem. 2015 Feb 26;58(4):1862-78.