ACT-660602 - ≥99% , CAS No.1646267-59-5

CAS: 1646267-59-5 Cat. No.: A646614 分子式: C₂₀H₂₀F₆N₈OS 分子量: 534.48

GRADE & PURITY ≥99%

Storage

Store at 2-8°C,Protected from light,Desiccated

Shipped In

Wet ice

概要

ACT-660602 is an orally active antagonist of chemokine receptor ( CXCR3 ) with an IC 50 value of 204 nM. ACT-660602 inhibits T-cell migration and shows efficacy in acute lung ingury model. ACT-660602 can be used for autoimmune diseases research

In Vitro

ACT-660602 shows selectivity to CXCR3 over hERG, with IC 50 s of 18 μM (hERG). ACT-660602 (112 nM; 6 h) inhibits cell migration and improves the metabolic stability. ACT-660602 (5, 20, 100 or 500 nM) displays an non-competitive binding mode to CXCL10 and CXCL11 in different concentration, with more stable IC 50 s. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Migration AssayCell Line: CD3/CD28-activated primary human T cells Concentration: 112 nM Incubation Time: 45 min Result: Inhibited cell migration.

In Vivo

ACT-660602 (1 μM; 6 h) intrinsic metabolic clearance (CLint) in human, rat, mouse liver microsomes (HLM, RLM, MLM) . ACT-660602 (30 mg/kg; p.o.; once daily) displays anti-inflammatory activity and exerts efficacy in the mouse model of acute lung ingury . Range for Pharmacokinetics of ACT-660602 Animal Route Dose (range) (mg/kg) C max (range) (ng/mL) T max (range) (h) AUC (range) (ng•h/mL) F (%) CL (range) (mL/min/kg) V ss (range) (L/kg) T 1/2 (range) (h) Dog p.o. 2 1380 1 20000 8 1.3 1.7 14.5 i.v. 0.5 1300-1450 0.5-2.0 10400-32000 / 0.6-3.0 1.6-1.7 6.3- Rat p.o. 2 1520 0.5 14000 80 1.9 1.1 7.1 i.v. 0.5 1250-1860 0.5-1.0 11600-15641 / 1.9-1.9 0.9-1.3 5.7-8.8 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: LPS-induced lung inflammation model (72 h post LPS challenge) Dosage: 30 mg/kg Administration: Oral gavage; once daily Result: Significantly reduced recruitment of the CXCR3+ CD8+ T cell in the bronchoalveolar lavage compartment.

Form:Solid

IC50& Target:CXCR3 204 nM (IC 50 )

Specifications

仕様と純度

≥99%

生化学的・生理学的メカニズム

ACT-660602 is an orally active antagonist of chemokine receptor ( CXCR3 ) with an IC 50 value of 204 nM. ACT-660602 inhibits T-cell migration and shows efficacy in acute lung ingury model. ACT-660602 can be used for autoimmune diseases research.

保管条件

Store at 2-8°C,Protected from light,Desiccated

入荷

Wet ice

この製品は冷冷この冷このこの製品の運送が必要です。地上およびその他の経済サービスは利用できません。

アクションタイプ

ANTAGONIST

純度

≥99%

名前と識別子

• 分子量: 534.48

化学的性質と物理的性質

• 溶解度: DMSO : 110 mg/mL (205.81 mM; Need ultrasonic)

よくある質問

What is the purity of this product?

This product is supplied at ≥99% purity (chemical assay). Lot-specific values are stated on the Certificate of Analysis.

How should this product be stored?

Store at 2–8 °C, protected from light, desiccated. Keep the container tightly closed with desiccant — the material is moisture-sensitive.

How is this product shipped?

This product ships chilled on wet ice. Unpack on arrival and transfer it to the storage condition stated above.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 1646267-59-5, the molecular formula is C20H20F6N8OS, and the molecular weight is 534.48 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.