| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| 2g |
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| 5g |
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| 10g |
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| Other Sizes |
Purity: ≥98%
| Targets |
Irbesartan HCl is a non-peptide angiotensin II type 1 (AT1) receptor blocker (ARB). It selectively and competitively blocks the binding of angiotensin II to the AT1 receptor, thereby inhibiting the vasoconstrictor and aldosterone-secreting effects of angiotensin II. This leads to vasodilation, reduced blood pressure, and improved blood flow. Irbesartan HCl has an IC50 of 1.3 nM for the AT1 receptor. It is used mainly for the treatment of hypertension and diabetic nephropathy. By blocking the AT1 receptor, Irbesartan HCl modulates the renin-angiotensin system.
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| ln Vitro |
Irbesartan hydrochloride (20 μM, 3 h) decreases Th22 cell chemotaxis in vitro[1].
Irbesartan hydrochloride (0 μM, 20 μM, 40 μM and 60 μM) inhibits the differentiation of Th22 cells in vitro[1]. Irbesartan hydrochloride (20 μM) inhibits the proinflammatory response of TECs related to Th22 cells in vitro[1]. In vitro, Irbesartan HCl is a highly potent and specific antagonist of the angiotensin II type 1 (AT1) receptor, with an IC50 of 1.3 nM. It selectively and competitively blocks the binding of angiotensin II to the AT1 receptor. The compound's high affinity for the AT1 receptor underlies its potent antihypertensive effects. Its in vitro activity is characterized by its ability to inhibit angiotensin II-induced vasoconstriction and aldosterone secretion in cellular and tissue models. |
| ln Vivo |
Irbesartan hydrochloride (oral gavage; 50 mg/kg/d; once daily) lowers serum IL-22 levels and Th22 lymphocytosis in Ang II-infused mice[1].
Irbesartan hydrochloride (oral gavage; 50 mg/kg/d; once daily) has clear renoprotective effects [1]. Irbesartan hydrochloride (oral gavage; 50 mg/kg/d; once daily) alleviates both systemic inflammation and renal fibrosis in hypertension mice induced by Ang II[1]. Irbesartan hydrochloride (20 μM; for 3 h) can reduce the number of Th22 cells recruited and the secretion of IL-22, possibly by preventing chemotaxis in mice with hypertensive renal injury[1]. In vivo, Irbesartan HCl is an orally active Ang II type 1 (AT1) receptor blocker (ARB). It is used mainly for the treatment of hypertension and diabetic nephropathy. The compound can relax blood vessels, lower blood pressure, and increase the supply of blood and oxygen to the heart. Its in vivo efficacy is well-established from clinical use. Irbesartan HCl is used as an adjunct to dietary therapy to prevent cardiovascular events. The compound's oral bioavailability supports its use in once-daily dosing. |
| Enzyme Assay |
Irbesartan s an extremely strong and selective antagonist of the angiotensin II type 1 (AT1) receptor with IC50 of 1.3 nM.
In vitro enzyme/receptor binding assays for Irbesartan HCl typically involve measuring its binding affinity to the angiotensin II type 1 (AT1) receptor. Radioligand binding assays using membrane preparations expressing the AT1 receptor are performed to determine the IC50. Irbesartan HCl shows an IC50 of 1.3 nM for the AT1 receptor. These assays confirm the compound's mechanism of action as a selective AT1 receptor antagonist. The compound's selectivity over other receptor subtypes is also assessed. |
| Cell Assay |
Irbesartan treatment significantly increases the expression of the adipogenic marker gene adipose protein 2 (aP2) in 3T3-L1 cells in a concentration-dependent manner. The induction increases by 3.3 times at a concentration of 10 μM, with an EC50 of 3.5 μM. Irbesartan (10 μM) significantly increases the transcriptional activity of peroxisome proliferator-activated receptor-γ (PPARγ) by 3.4 times, even in the absence of its ability to block AT1 receptors. In rat vascular smooth muscle cells, pretreatment with irbesartan (~10 μM) reduces angiotensin II-induced apoptosis by inhibiting angiotensin II internalization in a concentration-dependent way.
In vitro cellular assays for Irbesartan HCl typically involve measuring its effects on angiotensin II-induced cellular responses, such as calcium mobilization or inositol phosphate production, in cells expressing the AT1 receptor. The compound inhibits angiotensin II-induced signaling in a concentration-dependent manner. Its IC50 of 1.3 nM for the AT1 receptor is confirmed in these cellular assays. These cell-based studies demonstrate the compound's functional antagonism at the AT1 receptor. |
| Animal Protocol |
Dissolved in water by neutralization with a stoichiometric equivalent of KOH, or dissolved in saline by neutralization with a stoichiometric equivalent of L-arginine; 1 mg/kg; oral gavage Male Sprague-Dawley rats and female cynomolgus monkeys (Macaca fascicularis) injected (iv) with angiotensin II (AII) |
| ADME/Pharmacokinetics |
Irbesartan HCl is an orally active compound with favorable pharmacokinetic properties. It is rapidly absorbed after oral administration and has a bioavailability of approximately 60-80%. The compound is metabolized in the liver, primarily by CYP2C9, and is excreted in bile and urine. Its half-life is approximately 11-15 hours, supporting once-daily dosing. Irbesartan HCl's pharmacokinetic profile is well-characterized from its clinical use as an antihypertensive agent. The compound's oral bioavailability supports its use in once-daily dosing.
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| Toxicity/Toxicokinetics |
Irbesartan HCl is a well-tolerated medication with a favorable safety profile. Common adverse effects include dizziness, headache, and gastrointestinal disturbances. As with other ARBs, it may cause hyperkalemia and renal impairment in susceptible patients. The compound is contraindicated in patients with hypersensitivity to ARBs and in pregnant women. Its safety profile is well-established from extensive clinical use. Irbesartan HCl is for research use only and is not approved for human therapeutic use in many applications.
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| References | |
| Additional Infomation |
Drug Indication
Treatment of essential hypertension. As part of an antihypertensive medication regimen, for the treatment of kidney disease in patients with both hypertension and type 2 diabetes. Irbesartan HCl (CAS# 329055-23-4), also known as SR-47436 hydrochloride or BMS-186295, is a novel, highly potent, and specific angiotensin II type 1 (AT1) receptor antagonist with an IC50 of 1.3 nM. It is an orally active Ang II type 1 (AT1) receptor blocker (ARB). Irbesartan HCl is principally employed to manage hypertension and diabetic nephropathy. It can relax blood vessels, lower blood pressure, and increase the supply of blood and oxygen to the heart. The compound is for research use only and is not approved for human therapeutic use in many applications. |
| Molecular Formula |
C25H29CLN6O
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| Molecular Weight |
464.998
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| Exact Mass |
464.209
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| Elemental Analysis |
C, 64.58; H, 6.29; Cl, 7.62; N, 18.07; O, 3.44
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| CAS # |
329055-23-4
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| Related CAS # |
Irbesartan; 138402-11-6
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| PubChem CID |
11568906
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| Appearance |
Solid powder
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| LogP |
4.952
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
33
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| Complexity |
682
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| Defined Atom Stereocenter Count |
0
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| SMILES |
Cl.O=C1C2(CCCC2)N=C(CCCC)N1CC1C=CC(C2=CC=CC=C2C2N=NNN=2)=CC=1
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| InChi Key |
ZUYFSRQJPNUOQU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H28N6O.ClH/c1-2-3-10-22-26-25(15-6-7-16-25)24(32)31(22)17-18-11-13-19(14-12-18)20-8-4-5-9-21(20)23-27-29-30-28-23;/h4-5,8-9,11-14H,2-3,6-7,10,15-17H2,1H3,(H,27,28,29,30);1H
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| Chemical Name |
2-butyl-3-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]-1,3-diazaspiro[4.4]non-1-en-4-one;hydrochloride
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| Synonyms |
SR-47436; BMS 186295; BMS186295; SR47436; Avapro; Aprovel; KarveaIrbesartan HCl; Irbesartan hydrochloride; BMS-186295; SR 47436
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| HS Tariff Code |
2934.99.03.00
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| 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)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1505 mL | 10.7527 mL | 21.5054 mL | |
| 5 mM | 0.4301 mL | 2.1505 mL | 4.3011 mL | |
| 10 mM | 0.2151 mL | 1.0753 mL | 2.1505 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.
Calculation results
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.
(2) Be sure to add the solvent(s) in order.
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