| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
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| 100mg |
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| 250mg | |||
| 500mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
AT2 Receptor ( Ki = 0.4 nM ); AT1 Receptor ( Ki > 10 μM )
AT2 Agonist C21 targets the angiotensin II type 2 receptor (AT2R). By selectively activating AT2R, it counteracts the effects of angiotensin II mediated through the AT1 receptor. AT2R activation leads to vasodilation, reduced inflammation, and promotion of tissue repair and regeneration. The compound is a valuable tool for studying the role of AT2R in various physiological and pathological processes. |
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| 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.
In vitro, AT2 Agonist C21 activates the AT2 receptor, leading to downstream signaling events such as activation of protein phosphatases and inhibition of MAP kinase pathways. Its selective activation of AT2R over AT1R has been characterized in receptor binding and functional assays. The compound is used to study AT2R-mediated cellular responses. |
| 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].
In vivo, AT2 Agonist C21 has been studied in animal models of cardiovascular and renal diseases. It has shown beneficial effects such as vasodilation, reduced blood pressure, and protection against tissue injury. Its activation of AT2R promotes tissue repair and regeneration, making it a potential therapeutic agent for various conditions. |
| Enzyme Assay |
The activity of AT2 Agonist C21 can be assessed using radioligand binding assays with membranes expressing the AT2 receptor. The displacement of a radiolabeled AT2 ligand is measured to determine the binding affinity. Functional assays measuring AT2R-mediated signaling, such as activation of protein phosphatases, can also be used.
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| Cell Assay |
To evaluate the cellular effects of AT2 Agonist C21, cells expressing the AT2 receptor are treated with the compound. The activation of downstream signaling pathways is assessed by Western blotting. The effects on cell proliferation, migration, and inflammation are measured.
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| Animal Protocol |
In vivo studies with AT2 Agonist C21 typically involve administration to animal models via oral or intravenous routes. In models of hypertension, the compound's effects on blood pressure are assessed. In models of tissue injury, its effects on repair and regeneration are evaluated.
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| ADME/Pharmacokinetics |
AT2 Agonist C21 (M24) has a CAS number of 477775-14-7. It is a selective AT2 receptor agonist. The compound is soluble in DMSO and other organic solvents. The purity is typically ≥98%. It should be stored according to the manufacturer's instructions.
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| Toxicity/Toxicokinetics |
Specific toxicology data for AT2 Agonist C21 are not extensively detailed in the available literature. However, its use in animal models at effective doses suggests a degree of tolerability. As with all research compounds, standard safety precautions should be taken when handling AT2 Agonist C21. It is intended for research use only and is not for human consumption.
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| References |
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| Additional Infomation |
AT2 Agonist C21 (M24) is a selective angiotensin II type 2 receptor agonist. It activates the AT2 receptor, leading to vasodilation, anti-inflammatory, and tissue repair effects. It is a research tool for studying the role of AT2R in cardiovascular and renal diseases.
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| Molecular Formula |
C23H29N3O4S2
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|---|---|
| Molecular Weight |
475.6241
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| Exact Mass |
475.159
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| Elemental Analysis |
C, 58.08; H, 6.15; N, 8.83; O, 13.46; S, 13.48
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| CAS # |
477775-14-7
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| PubChem CID |
9804984
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| Appearance |
White to yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Index of Refraction |
1.615
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| LogP |
4.93
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
32
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| Complexity |
690
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S1C(=C(C2C([H])=C([H])C(C([H])([H])N3C([H])=NC([H])=C3[H])=C([H])C=2[H])C([H])=C1C([H])([H])C([H])(C([H])([H])[H])C([H])([H])[H])S(N([H])C(=O)OC([H])([H])C([H])([H])C([H])([H])C([H])([H])[H])(=O)=O
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| InChi Key |
XTEOJPUYZWEXFI-UHFFFAOYSA-N
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| 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)
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| Chemical Name |
butyl N-[3-[4-(imidazol-1-ylmethyl)phenyl]-5-(2-methylpropyl)thiophen-2-yl]sulfonylcarbamate
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| Synonyms |
M 24; Buloxibutid; AT2 Agonist C21; C21; M24; M-24; C-21; C 21; AT2 receptor agonist C21
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| HS Tariff Code |
2934.99.9001
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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) |
DMSO: ~100 mg/mL (~210.3 mM)
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|---|---|
| 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. View More
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. |
| 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.
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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