Acifran
Based on 1 publication(s) in Google Scholar
Acifran (AY 25712) is an orally active, full GPR109A and GPR109B agonist and hypolipidemic agent. Acifran reduces Forskolin (HY-15371)-induced cAMP elevation, triggers ERK1/ERK2 phosphorylation, and inhibits lipolysis in adipose tissue through Gi-coupled GPCR activation. Acifran is used for research on atherosclerosis, hyperlipidemia, and type 2 diabetes.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 99.03%
- CAS 番号: 72420-38-3
- 分子式: C12H10O4
- 分子量:218.21
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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HY-107581
MK-1903GPR109a/HCAR2 Agonist -
HY-107579R
Acifran (Standard)Reference Standard -
HY-107580
GPR109 receptor agonist-1GPR109b Receptor Agonist -
HY-W015560
3,5-Dihydroxybenzoic acidGPR81 Agonist -
HY-100976
LUF6283HCA(2) Agonist -
HY-B0283
AcipimoxAntilipolytic Agent -
HY-W015560R
3,5-Dihydroxybenzoic acid (Standard)GPR81 Agonist -
HY-119222
GSK256073GPR109A Agonist -
HY-107581R
MK-1903 (Standard)Reference Standard -
HY-B0283R
Acipimox (Standard)Antilipolytic Agent
MedChemExpress（MCE）の使用を引用している文献 Acifran
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生物活性
製品説明
IC50 & Target
[3]|
ERK1 |
ERK2 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO-K1 | EC50 |
160 nM
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Phosphorylation of ERK1/ERK2 in CHO-K1 cells stably expressing HM74A incubated for 5 mins followed by ELISA.
Phosphorylation of ERK1/ERK2 in CHO-K1 cells stably expressing HM74A incubated for 5 mins followed by ELISA.
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16389067 |
| CHO-K1 | EC50 |
316 nM
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Phosphorylation of ERK1/ERK2 in CHO-K1 cells stably expressing HM74 incubated for 5 mins followed by ELISA.
Phosphorylation of ERK1/ERK2 in CHO-K1 cells stably expressing HM74 incubated for 5 mins followed by ELISA.
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16389067 |
体外実験
Acifran is a full agonist of GPR109a, with an EC50 of 1.3 μM in the cAMP whole-cell assay and an EC50 of 4.2 μM for GPR109b[1].
Acifran (10-50 μg/mL) shows weak binding to rat and dog serum proteins, and significantly displaces protein-bound Warfarin (HY-B0687) only in dog serum[2].
Acifran (5 min) activates ERK1/ERK2 phosphorylation with an EC50 of 160 nM in CHO-K1 cells expressing HM74A and an EC50 of 316 nM in CHO-K1 cells expressing HM74 [3].
Acifran (1 μM) induces strong phosphorylation of p-ERK1/ERK2 in CHO-K1 cells expressing HM74A and HM74, and this effect is completely inhibited by Pertussis toxin[3].
Acifran (20-200 μM; 5 min) induces phosphorylation of p-ERK1/ERK2 in CHO-K1 cells stably expressing HM74A[3].
Acifran (20-200 μM; 5 min) activates ERK1/ERK2 phosphorylation in CHO-K1 cells stably expressing HM74[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:CHO-K1 cells stably expressing HM74A or HM74
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Concentration:9-point log10 scale
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Incubation Time:5 min
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Result:Yielded an EC50 of 160 nM for HM74A.
Yielded an EC50 of 316 nM for HM74.
Showed a modest effect on phosphorylation of ERK1/ERK2 in parental CHO-K1 cells only at 100 μM.
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Cell Line:CHO-K1 cells stably expressing HM74A
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Concentration:20-200 μM
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Incubation Time:5 min
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Result:Elicited p-ERK1/ERK2 phosphorylation at both 20 μM and 200 μM, with a robust signal appearing at both concentrations.
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Cell Line:CHO-K1 cells stably expressing HM74
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Concentration:20-200 μM
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Incubation Time:5 min
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Result:Elicited phosphorylation of ERK1/ERK2 at both 20 μM and 200 μM, with robust activation observed even at 20 μM.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (male, 175-200 g, fructose-fed)[3]
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Dosage:1, 2.5, 5, 10, 15 mg/kg
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Administration:p.o.; single dose
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Result:Decreased serum triglycerides dose-dependently by 39% at 1 mg/kg, 44% at 2.5 mg/kg, 49% at 5 mg/kg, 57% at 10 mg/kg, and 61% at 15 mg/kg versus untreated control.
化学情報
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CAS 番号 72420-38-3
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性状 Solid
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分子量 218.21
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分子式 C12H10O4
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Color Off-white to light yellow
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SMILES
O=C(C(OC1(C)C2=CC=CC=C2)=CC1=O)O
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別名
アシフラン; AY 25712
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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iScience
Comparative analysis reveals molecular adaptation of mammalian HCA2 to microbial metabolites. [Abstract]2026 May 22;29(6):116030. PMID: 42221821
溶剤 & 溶解度
体外:
DMSO : 125 mg/mL (572.84 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (292 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Jung JK, et al. Analogues of acifran: agonists of the high and low affinity niacin receptors, GPR109a and GPR109b. Journal of medicinal chemistry. 2007 Apr 05;50(7):1445-8. [Content Brief]
[2]. Cayen MN, et al. The metabolic disposition of acifran, a new antihyperlipidemic agent, in rats and dogs. Xenobiotica; the fate of foreign compounds in biological systems. 1986 Mar;16(3):251-63. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 4.5827 mL | 22.9137 mL | 45.8274 mL | 114.5685 mL |
| 5 mM | 0.9165 mL | 4.5827 mL | 9.1655 mL | 22.9137 mL | |
| 10 mM | 0.4583 mL | 2.2914 mL | 4.5827 mL | 11.4569 mL | |
| 15 mM | 0.3055 mL | 1.5276 mL | 3.0552 mL | 7.6379 mL | |
| 20 mM | 0.2291 mL | 1.1457 mL | 2.2914 mL | 5.7284 mL | |
| 25 mM | 0.1833 mL | 0.9165 mL | 1.8331 mL | 4.5827 mL | |
| 30 mM | 0.1528 mL | 0.7638 mL | 1.5276 mL | 3.8190 mL | |
| 40 mM | 0.1146 mL | 0.5728 mL | 1.1457 mL | 2.8642 mL | |
| 50 mM | 0.0917 mL | 0.4583 mL | 0.9165 mL | 2.2914 mL | |
| 60 mM | 0.0764 mL | 0.3819 mL | 0.7638 mL | 1.9095 mL | |
| 80 mM | 0.0573 mL | 0.2864 mL | 0.5728 mL | 1.4321 mL | |
| 100 mM | 0.0458 mL | 0.2291 mL | 0.4583 mL | 1.1457 mL |
Acifran 関連分類
HY-107579 関連分類
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