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Cat. No.: HY-114953

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BMS-248360

BMS-248360 is a potent and orally active dual antagonist of both angiotensin II receptor (AT1) and endothelin A (ET_A) receptor, with K_is of 10 nM and 1.9 nM for hAT1 and hETA receptor, respectively. BMS-248360 displays hypertensive effects.

For research use only. We do not sell to patients.

CAS No.: 254737-87-6
Formula: C₃₆H₄₅N₅O₅S
Molecular Weight:659.84

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (284 KB)

BMS-248360 Chemical Structure

CAS No.: 254737-87-6

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

Ki: 10 nM (hAT1), 1.9 nM (hETA receptor), 6.0 nM (rAT1), 1.9 nM(rET_A receptor)^[1]

All Angiotensin Receptor Isoforms :

All Endothelin Receptor Isoforms :

ET_A
ET_B

Cellular Effect

Cell Line	Type	Value	Description	References
CHO-K1	IC₅₀	2 nM Compound: BMS-248360	Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis Displacement of 125I-labeled endothelin 1 from human ETA receptor expressed in CHO-K1 cells incubated for 4 hrs by gamma counting analysis	10.1039/C4MD00499J

In Vitro

BMS-248360 shows activity against rat AT1 and rat ET_A receptor, with K_is of 6.0 nM and 1.9 nM, respectively^[1].
BMS-248360 shows no activity against AT2 and ET_B receptor subtypes^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

BMS-248360 is found to be orally bioavailable in rats (%F=38) with excellent oral exposure (C_max)=3.1 µM) and reasonable elimination profile (T_1/2=5.5 hours)^[1].
BMS-248360 (30 µmol/kg, 100 µmol/kg; p.o.) blocks the hypertensive effects of intravenously administered AII^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Male Rats^[1]
Dosage:

30 µM/kg, 100 µM/kg
Administration:

Oral administration
Result:

Blocked the hypertensive effects of intravenously administered AII.

Animal Model:

Male Rats^[1]
Dosage:

10 µM/kg
Administration:

Oral administration
Result:

T_1/2= 5.5 hours

Chemical Information

CAS No. 254737-87-6
Molecular Weight 659.84
Formula C₃₆H₄₅N₅O₅S
SMILES

O=S(C1=CC=CC=C1C2=CC=C(CN3C(CCCC)=NC4(CCCC4)C3=O)C=C2CN5C(C(C)(C)CC5)=O)(NC6=C(C)C(C)=NO6)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (284 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Murugesan N, et al. Discovery of N-isoxazolyl biphenylsulfonamides as potent dual angiotensin II and endothelin A receptor antagonists. J Med Chem. 2002 Aug 29;45(18):3829-35. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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BMS-248360

All Angiotensin Receptor Isoforms

All Endothelin Receptor Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

BMS-248360 Related Classifications

HY-114953 Related Classifications