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GS-444217

Cat. No. M9229
GS-444217 Structure
Synonym:

ASK1-IN-1

Size Price Availability Quantity
2mg USD 275  USD275 In stock
5mg USD 437  USD437 In stock
25mg USD 1247  USD1247 In stock
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Quality Control
Biological Activity

GS-444217 reduces ASK1 phosphorylation and prevents the phosphorylation of MKK3/6, MKK4, p38, and JNK at concentrations of 0.3 μM and above with full suppression of ASK1 activity at 1 μM.

In vivo, GS-444217 reduces oxidative stress (OS)-induced ASK1 signaling in kidney and inhibits acute renal tubular injury in rats. GS-444217 (30 mg/kg) inhibits activation of ASK1, p38, and JNK in rat kidney. GS-444217 has an in vivo EC50 of approximately 1.6 μM for inhibiting the ASK1 pathway in rodent kidney.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 411.46
Formula C23H21N7O
CAS Number 1262041-49-5
Purity 99.92%
Solubility DMSO: 10 mg/mL
Storage at -20°C
References

[1] Liles JT, et al. J Clin Invest. ASK1 contributes to fibrosis and dysfunction in models of kidney disease.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: GS-444217, ASK1-IN-1 supplier, p38 MAPK, inhibitors

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