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TC-S 7001

Cat. No. M7388
TC-S 7001 Structure
Synonym:

ROCK inhibitor; TC-S 7001

Size Price Availability Quantity
5mg USD 330  USD330 In stock
10mg USD 530  USD530 In stock
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Quality Control & Documentation
Biological Activity

TC-S 7001 is a potent and highly selective ROCK inhibitor (IC50 values are 0.6 and 1.1 nM for ROCK1 and ROCK2, respectively). Exhibits >200-fold selectivity over TRK and FLT3 receptors, and >900-fold selectivity over a panel of other kinases and cardiovascular relevent enzymes and receptors. Reduces blood pressure in normotensive and hypertensive rats. Orally active.

Product Citations
Chemical Information
Molecular Weight 402.79
Formula C18H13ClF2N6O
CAS Number 867017-68-3
Form Solid
Solubility (25°C) DMSO 40.28 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
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] Gatley, et al. Eur J Pharmacol. 125I-labeled AM 251: a radioiodinated ligand which binds in vivo to mouse brain cannabinoid CB1 receptors.

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  Catalog
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Keywords: TC-S 7001, ROCK inhibitor; TC-S 7001 supplier, ROCK, inhibitors, activators


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