AT2 Agonist C21 (M24)

Alias: M 24; Buloxibutid; AT2 Agonist C21; C21; M24; M-24; C-21; C 21; AT2 receptor agonist C21
Cat No.:V11787 Purity: ≥98%
AT2 Agonist C21(M-24) is a novel, potent and selective agonist of angiotensin AT2 receptors with Ki values of 0.4 nM and >10 µM for the AT2 receptor and AT1 receptor, respectively.
AT2 Agonist C21 (M24) Chemical Structure CAS No.: 477775-14-7
Product category: Angiotensin Receptor
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

AT2 Agonist C21 (M-24) is a novel, potent and selective agonist of angiotensin AT2 receptors with Ki values of 0.4 nM and >10 µM for the AT2 receptor and AT1 receptor, respectively. It inhibits leukocyte adhesion and endothelial inflammation both in vivo and in vitro.

Biological Activity I Assay Protocols (From Reference)
Targets
AT2 Receptor ( Ki = 0.4 nM ); AT1 Receptor ( Ki > 10 μM )
ln Vitro
Buloxibutid stimulates p42/p44mapk, increases in vivo duodenal alkaline secretion in Sprague-Dawley rats, induces neurite cell outgrowth, and lowers the mean arterial blood pressure in anesthetized, spontaneously hypertensive rats. Its half-life in rats is estimated to be 4 hours.
ln Vivo
Buloxibutid has a bioavailability of 20-30% after oral administration, and its half-life in rats is estimated to be 4 hours. It can induce neurite cell growth, stimulate p42/p44mapk, and enhance duodenal alkaline secretion in Sprague-Dawley rats. and reduced mean arterial blood pressure in anesthetized spontaneously hypertensive rats [1].
References

[1]. Design, synthesis, and biological evaluation of the first selective nonpeptide AT2 receptor agonist. J Med Chem. 2004 Nov 18;47(24):5995-6008.

[2]. Angiotensin AT2-receptor stimulation improves survival and neurological outcome after experimental stroke in mice. J Mol Med (Berl). 2016;94(8):957-966.

[3]. Angiotensin AT2 Receptor is Anti-inflammatory and Reno-Protective in Lipopolysaccharide Mice Model: Role of IL-10. Front Pharmacol. 2021;12:600163.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C23H29N3O4S2
Molecular Weight
475.6241
Exact Mass
475.16
Elemental Analysis
C, 58.08; H, 6.15; N, 8.83; O, 13.46; S, 13.48
CAS #
477775-14-7
Appearance
Solid powder
SMILES
CCCCOC(=O)NS(=O)(=O)C1=C(C=C(S1)CC(C)C)C2=CC=C(C=C2)CN3C=CN=C3
InChi Key
XTEOJPUYZWEXFI-UHFFFAOYSA-N
InChi Code
InChI=1S/C23H29N3O4S2/c1-4-5-12-30-23(27)25-32(28,29)22-21(14-20(31-22)13-17(2)3)19-8-6-18(7-9-19)15-26-11-10-24-16-26/h6-11,14,16-17H,4-5,12-13,15H2,1-3H3,(H,25,27)
Chemical Name
butyl N-[3-[4-(imidazol-1-ylmethyl)phenyl]-5-(2-methylpropyl)thiophen-2-yl]sulfonylcarbamate
Synonyms
M 24; Buloxibutid; AT2 Agonist C21; C21; M24; M-24; C-21; C 21; AT2 receptor agonist C21
HS Tariff Code
2934.99.9001
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: ~100 mg/mL (~210.3 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.37 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.08 mg/mL (4.37 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.08 mg/mL (4.37 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.


 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.1025 mL 10.5126 mL 21.0252 mL
5 mM 0.4205 mL 2.1025 mL 4.2050 mL
10 mM 0.2103 mL 1.0513 mL 2.1025 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.

Calculator

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What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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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