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M1002 

Cat. No. M30650
M1002  Structure
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Biological Activity

M1002 is a hypoxia-inducible factor-2 (HIF-2) agonist, and can enhance the expression of HIF-2 target genes. M1002 shows synergy with prolyl-hydroxylase domain (PHD) inhibitors.

Chemical Information
Molecular Weight 394.29
Formula C15H8F6N2O2S
CAS Number 823830-85-9
Form Solid
Solubility (25°C) DMSO 50 mg/mL (ultrasonic and warming and heat to 60°C)
DMF 50 mg/mL (ultrasonic)
Storage Powder -20°C
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Yancheng Yu, et al. Eur J Med Chem. Insight into the binding mode of HIF-2 agonists through molecular dynamic simulations and biological validation

[2] Jonathan Gornall. BMJ. Big cannabis in the UK: is industry support for wider patient access motivated by promises of recreational market worth billions?

[3] Yanqing Miao, et al. Acta Crystallogr Sect E Struct Rep Online. Poly[(μ(5)-3,5-dinitro-benzoato)rubidium]

[4] Bing-Xin Liu, et al. Acta Crystallogr Sect E Struct Rep Online. Bis(2,2'-diamino-4,4'-bi-1,3-thia-zole-κN,N)bis-(nitrato-κO)lead(II) dihydrate

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Axl-IN-16 is a Axl inhibitor.

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HIF-2α-IN-9 is an inhibitor ofHIF-2α.

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PHD-IN-2 is a PHD antagonist (IC50: < 5 nM).

  Catalog
Abmole Inhibitor Catalog




Keywords: M1002  supplier, HIF, inhibitors, activators


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