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Tolvaptan

Cat. No. M3480
Tolvaptan Structure
Synonym:

OPC-41061

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
5mg USD 40  USD40 In stock
10mg USD 60  USD60 In stock
50mg USD 160  USD160 In stock
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Quality Control & Documentation
Biological Activity

Tolvaptan (OPC-41061)?is a selective, competitive arginine vasopressin receptor 2 antagonist with an IC50 of 1.28uM for the inhibition of AVP-induced platelet aggregation. Tolvaptan (OPC-41061) is used to treat hyponatremia (low blood sodium levels) associated with congestive heart failure, cirrhosis, and the syndrome of inappropriate antidiuretic hormone (SIADH). Tolvaptan (OPC-41061) is also in fast-track clinical trials for polycystic kidney disease. Treatment with t tolvaptan (OPC-41061) causes rapid and sustained body weight reductions concurrent with increases in urine output, improves and/or normalizes serum sodium in hyponatremic patients, reduces signs and symptoms of congestion and increases thirst. However, tolvaptan (OPC-41061) has not been shown to decrease heart failure re-hospitalization or mortality. As an adjunct to standard therapy, tolvaptan (OPC-41061) is unique in that it is virtually the only novel agent tested in patients hospitalized for acute heart failure syndrome (AHFS) to reach its primary end point for short-term efficacy without causing deleterious side effects.

Product Citations
Chemical Information
Molecular Weight 448.94
Formula C26H25ClN2O3
CAS Number 150683-30-0
Solubility (25°C) DMSO 80 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] Takuya Adachi, et al. Management of Cirrhotic Ascites under the Add-on Administration of Tolvaptan

[2] Olivier Bonny, et al. Clinical use of tolvaptan: a 2021 review

[3] Hannah A Blair. Tolvaptan: A Review in Autosomal Dominant Polycystic Kidney Disease

[4] Fouad T Chebib, et al. A Practical Guide for Treatment of Rapidly Progressive ADPKD with Tolvaptan

[5] Greg L Plosker. Tolvaptan

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Keywords: Tolvaptan, OPC-41061 supplier, Vasopressin Receptor, inhibitors, activators


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