Irbesartan (SR-47436; BMS-186295)

Alias: BMS-186295, SR-47436;BMS 186295, SR 47436; BMS186295, SR47436; Avapro, Aprovel, Karvea
Cat No.:V1776 Purity: ≥98%
Irbesartan (formerly known as SR47436; BMS186295;SR-47436; BMS-186295; Avapro, Aprovel, Karvea) is a highly potent and specific angiotensin II type 1 (AT II-1) receptor antagonist/ARB approved as an antihypertension drug.
Irbesartan (SR-47436; BMS-186295) Chemical Structure CAS No.: 138402-11-6
Product category: RAAS
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
10mg
50mg
100mg
250mg
500mg
1g
2g
Other Sizes

Other Forms of Irbesartan (SR-47436; BMS-186295):

  • Irbesartan D4
  • Irbesartan HCl
  • Irbesartan-d6-1 (irbesartan-d6-1; irbesartan-d6-1)
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Irbesartan (formerly known as SR47436; BMS186295; SR-47436; BMS-186295; Avapro, Aprovel, Karvea) is a highly potent and specific angiotensin II type 1 (AT II-1) receptor antagonist/ARB approved as an antihypertension drug. It inhibits AT II-1 with IC50 of 1.3 nM. Irbesartan is primarily used for the treatment of hypertension. It acts by selectively and competitively blocking the binding of angiotensin II to the angiotensin I receptor. Angiotensin II stimulates aldosterone synthesis and secretion by adrenal cortex, which decreases the excretion of sodium and increases the excretion of potassium. Angiotensin II also acts as a vasoconstrictor in vascular smooth muscle.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
In vitro, irbesartan (20 μM, 3 h) decreases Th22 cell chemotaxis[1]. In vitro, irbesartan (0 μM, 20 μM, 40 μM, and 60 μM) inhibits the development of Th22 cells[1]. In vitro, TECs' proinflammatory response associated to Th22 cells is inhibited by irbesartan (20 μM)[1].
ln Vivo
In Ang II-infused rats, irbesartan (oral gavage; 50 mg/kg/d; once daily) lowers serum IL-22 levels and Th22 lymphocytosis[1]. Renoprotective benefits of irbesartan (oral gavage; 50 mg/kg/d; once daily) are evident[1]. In hypertension-induced rats, irbesartan (oral gavage; 50 mg/kg/d; once daily) reduces kidney fibrosis and systemic inflammation[1]. In hypertensive renal injury mice, irbesartan hydrochloride (20 μM) for three hours can reduce Th22 cell recruitment and IL-22 release, possibly by blocking chemotaxis[1].
Cell Assay
Cell Viability Assay[1]
Cell Types: CD4+ T cells
Tested Concentrations: 0, 20, 40 and 60 μM
Incubation Duration: 48 h
Experimental Results: Exerted no obvious effect on viability of CD4+T cells.
Animal Protocol
Animal/Disease Models: C57BL/6 mice[1]
Doses: 50 mg/kg
Route of Administration: po (oral gavage); 50 mg/kg /d; one time/day
Experimental Results: Displayed low Th22 cells and IL-22, exerted similar inhibitory effect on Th1 cell proportion and displayed diminished IL-22 level in kidney. Prevented BP elevation markedly and diminished urinary albumin/creatinine ratio, BUN and Scr. Repressed the expression of IL-1β, IL-6, TNF-α, α-SMA, FN and Col I and diminished the extent of fibrosis.

Animal/Disease Models: C57BL/6 mice[1]
Doses: 20 μM
Route of Administration: 20 μM; for 3 h
Experimental Results: Downregulated renal CCL20, CCL22 and CCL27 concentrations.
References
[1]. Schupp M, et al. Angiotensin type 1 receptor blockers induce peroxisome proliferator-activated receptor-gamma activity. Circulation. 2004 May 4;109(17):2054-7. Epub 2004 Apr 26.
[2]. Ruiz E, et al. Importance of intracellular angiotensin II in vascular smooth muscle cell apoptosis: inhibition by the angiotensin AT1 receptor antagonist irbesartan. Eur J Pharmacol. 2007 Jul 19;567(3):231-9. Epub 2007 Apr 6.
[3]. Yong Zhong, et al. Irbesartan may relieve renal injury by suppressing Th22 cells chemotaxis and infiltration in Ang II-induced hypertension. Int Immunopharmacol
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C25H28N6O
Molecular Weight
428.53
CAS #
138402-11-6
SMILES
O=C1C2(C([H])([H])C([H])([H])C([H])([H])C2([H])[H])N=C(C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H])N1C([H])([H])C1C([H])=C([H])C(C2=C([H])C([H])=C([H])C([H])=C2C2N=NN([H])N=2)=C([H])C=1[H]
Synonyms
BMS-186295, SR-47436;BMS 186295, SR 47436; BMS186295, SR47436; Avapro, Aprovel, Karvea
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 4 mg/mL (9.3 mM)
Water:<1 mg/mL
Ethanol: 3 mg/mL (7.0 mM)
Solubility (In Vivo)
30% PEG400+0.5% Tween80+5%Propylene glycol: 30 mg/mL
 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.3336 mL 11.6678 mL 23.3356 mL
5 mM 0.4667 mL 2.3336 mL 4.6671 mL
10 mM 0.2334 mL 1.1668 mL 2.3336 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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