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Chemical Structure| 150375-75-0 Chemical Structure| 150375-75-0

Structure of SR 49059
CAS No.: 150375-75-0

Chemical Structure| 150375-75-0

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SR49059 is a potent and selective non-peptide vasopressin V1A receptor antagonist which is devoid of agonist activity. SR49059 displays high affinity and efficacy at both rat (Ki = 1.6 nM) and human (Ki = 1.1 - 6.3 nM) V1A receptors and potently antagonizes arginine vasopressin-induced effects in vitro (IC50 = 3.7 nM for inhibition of human platelet aggregation) and is orally active in vivo.

Synonyms: Relcovaptan

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Product Details of SR 49059

CAS No. :150375-75-0
Formula : C28H27Cl2N3O7S
M.W : 620.50
SMILES Code : O=C([C@H]1N(C([C@@H]2N(S(=O)(C3=CC=C(OC)C(OC)=C3)=O)C4=C(C=C(Cl)C=C4)[C@@]2(C5=CC=CC=C5Cl)O)=O)CCC1)N
Synonyms :
Relcovaptan
MDL No. :MFCD00922133

Safety of SR 49059

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H317
Precautionary Statements:P280-P305+P351+P338

Related Pathways of SR 49059

GPCR

Isoform Comparison

Biological Activity

Description
SR 49059 is a potent, orally active, and selective antagonist of the vasopressin V1a receptor, with a Ki value of 1.4 nM[1].

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Wistar rats Mild thermal dehydration model Intraperitoneal osmotic pumps 0.64 mg/day Continued for 2 weeks Evaluate the roles of V1a and V2 receptors in renal damage caused by heat stress dehydration followed by rehydration with fructose-containing beverages. Results showed that independent blockade of either V1a or V2 receptors prevented renal damage, reduced oxidative stress, and decreased plasma cortisol and systemic inflammation. PMC6888540

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.61mL

0.32mL

0.16mL

8.06mL

1.61mL

0.81mL

16.12mL

3.22mL

1.61mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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