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RO 46-8443

Cat. No. M10916
RO 46-8443 Structure
Size Price Availability Quantity
1mg USD 50  USD50 In stock
5mg USD 120  USD120 In stock
10mg USD 200  USD200 In stock
25mg USD 365  USD365 In stock
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Quality Control & Documentation
Biological Activity

RO 46-8443 is the first non-peptide endothelin ETB receptor selective antagonist. RO 46-8443 displays up to 2000-fold selectivity for ETB receptors both in terms of binding inhibitory potency and functional inhibition.

Chemical Information
Molecular Weight 609.69
Formula C31H35N3O8S
CAS Number 175556-12-4
Solubility (25°C) DMSO ≥ 5 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] Cludio L Guimares, et al. Clin Sci (Lond). Endothelin ET(B) receptor-mediated mechanisms involved in oleic acid-induced acute lung injury in mice

[2] Z Ming, et al. Hypertension. Endothelin-dependent tone limits acetylcholine-induced dilation of resistance coronary vessels after blockade of NO formation in conscious dogs

[3] M Clozel, et al. FEBS Lett. The role of ETB receptors in normotensive and hypertensive rats as revealed by the non-peptide selective ETB receptor antagonist Ro 46-8443

[4] V Breu, et al. FEBS Lett. In vitro characterisation of Ro 46-8443, the first non-peptide antagonist selective for the endothelin ETB receptor

[5] M Clozel, et al. J Cardiovasc Pharmacol. Are there different ETB receptors mediating constriction and relaxation?

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Keywords: RO 46-8443 supplier, Endothelin Receptor, inhibitors, activators


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