4-IsoxazolecarboxaMide, 3-(2-chlorophenyl)-N-(4-chlorophenyl)-N,5-diMethyl-
- CAS No.
- 1197300-24-5
- Chemical Name:
- 4-IsoxazolecarboxaMide, 3-(2-chlorophenyl)-N-(4-chlorophenyl)-N,5-diMethyl-
- Synonyms
- CCDC;TGR5;CS-1017;MDK00245;TGR5 Receptor Agonist;CCDC(TGR5-Receptor-Agonist);TGR5 Receptor Agonist, >=98%;TGR5 Receptor Agonist(isoxazole);TGR5 Receptor Agonist, 10 mM in DMSO;BENZYL (4-CHLORO-1H-PYRROLO[2,3-B]PYRIDIN-1-YL)ACETATE
- CBNumber:
- CB92627077
- Molecular Formula:
- C18H14Cl2N2O2
- Molecular Weight:
- 361.22
- MDL Number:
- MFCD17169972
- MOL File:
- 1197300-24-5.mol
- MSDS File:
- SDS
| Boiling point | 541.8±50.0 °C(Predicted) |
|---|---|
| Density | 1.346±0.06 g/cm3(Predicted) |
| storage temp. | 2-8°C |
| solubility | DMF: 50 mg/ml; DMSO: 50 mg/ml; DMSO:PBS (pH 7.2) (1:4): 0.2 mg/ml; Ethanol: 30 mg/ml |
| form | A crystalline solid |
| pka | -0.52±0.50(Predicted) |
| color | White to off-white |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
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|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Warning | |||||||||
| Hazard statements | H302-H315-H319-H332-H335 | |||||||||
| Precautionary statements | P261-P280-P305+P351+P338 | |||||||||
| NFPA 704 |
|
4-IsoxazolecarboxaMide, 3-(2-chlorophenyl)-N-(4-chlorophenyl)-N,5-diMethyl- price More Price(26)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Cayman Chemical | 16291 | TGR5 Receptor Agonist ≥98% | 1197300-24-5 | 1mg | $32 | 2024-03-01 | Buy |
| Cayman Chemical | 16291 | TGR5 Receptor Agonist ≥98% | 1197300-24-5 | 5mg | $122 | 2024-03-01 | Buy |
| Cayman Chemical | 16291 | TGR5 Receptor Agonist ≥98% | 1197300-24-5 | 10mg | $214 | 2024-03-01 | Buy |
| Cayman Chemical | 16291 | TGR5 Receptor Agonist ≥98% | 1197300-24-5 | 25mg | $456 | 2024-03-01 | Buy |
| Usbiological | T3662-50 | TGR5 Receptor Agonist | 1197300-24-5 | 5mg | $493 | 2021-12-16 | Buy |
4-IsoxazolecarboxaMide, 3-(2-chlorophenyl)-N-(4-chlorophenyl)-N,5-diMethyl- Chemical Properties,Uses,Production
Description
TGR5 receptor agonist is an agonist of the bile acid G protein-coupled receptor TGR5 (EC50s = 31.6-158.5 nM in cell-based assays). It stimulates cAMP formation in HEK293 cells expressing TGR5 (EC50 = 2.3 pM). TGR5 receptor agonist (1 mg/kg) increases glucagon-like peptide 1 (GLP-1) secretion and decreases glucose levels in the hepatic portal vein in dogs when administered in combination with glucose. It also inhibits the cytochrome P450 (CYP) isozymes CYP2C19 and CYP3A4 (IC50s = 316.2 and 1,259 nM, respectively).
Uses
TGR5 Receptor Agonist (CCDC), a potent Takeda G protein-coupled receptor 5 (TGR5; GPCR19) agonist, shows improved potency in the U2-OS cells and melanophore cells with pEC50s of 6.8 and 7.5, respectively. TGR5 Receptor Agonist can induce peripheral and central hypersensitivity to bladder distension in mice, and increase intracellular Ca2+ concentration. TGR5 Receptor Agonist can also reduces food intake and improves insulin responsiveness, in diet-induced obese mice. TGR5 Receptor Agonist can be used to research diabetes, bladder hypersensitivity and anti-obesity[1][2][3][4].
in vivo
TGR5 Receptor Agonist (CCDC) activates directly a sub-population of bladder-innervating dorsal root ganglia (DRG) neurons and a small percentage of non-neuronal cells in Trpv1-/- mice[2].
?
TGR5 Receptor Agonist (CCDC) (2?or 5 μg; ICV) reduces food intake and body weight in diet-induced obese mice[3].
| Animal Model: | Female C57BL/6J mice [12-18 weeks; TRPV1 knockout (trpv1-/-), TRPA1 knockout (trpa1-/-), or TGR5 knockout (Gpbar1-/-)][2] |
| Dosage: | 100 μM, 100 μL |
| Administration: | Infused gently, to fill but not fully distend the bladder, and allowed to incubate for 5 min |
| Result: | Activated directly a sub-population of bladder-innervating dorsal root ganglia (DRG) neurons in Trpv1-/- mice, also activated a small percentage of non-neuronal cells. Increased intracellular Ca2+ in bladder-innervating DRG neurons. Increased intracellular Ca2+ in a small proportion of non-neuronal cells. |
| Animal Model: | Male C57BL/6J mice (obese induced by high-fat diet)[3] |
| Dosage: | 2?or 5 μg at a volume of 0.2 μL per brain side and a rate of 0.6 μL/min |
| Administration: | ICV (acute intra-hypothalamic experiment) |
| Result: | Significantly reduced food intake over time, with a robust reduction in 24 h food intake and body weight gain. |
| Animal Model: | Male C57BL/6J mice (obese induced by high-fat diet; implanted with micro-osmotic pumps that were filled with CCDC)[3] |
| Dosage: | 5 μg/day; 91.9 μL, pumping rate of 0.09 μL/h |
| Administration: | ICV; for 4 weeks (chronic experiment) |
| Result: | Reduced food intake and improved insulin responsiveness. Increased energy expenditure during the dark phase. Increased mRNA expression of β1, 2, and 3 adrenoreceptors (Adrb1, Adrb2, and Adrb3) in the epidydimal white adipose tissue, and increased Dio2 (the gene expressing the enzyme D2) in brown adipose tissue. |
References
[1] Evans KA, et al. Discovery of 3-aryl-4-isoxazolecarboxamides as TGR5 receptor agonists. J Med Chem. 2009 Dec 24;52(24):7962-5. DOI:10.1021/jm901434t
[2] Caldwell A, Grundy L, Harrington AM, Garcia-Caraballo S, Castro J, Bunnett NW, Brierley SM. TGR5 agonists induce peripheral and central hypersensitivity to bladder distension. Sci Rep. 2022 Jun 15;12(1):9920. DOI:10.1038/s41598-022-14195-w
[3] Castellanos-Jankiewicz A, et al. Hypothalamic bile acid-TGR5 signaling protects from obesity. Cell Metab. 2021 Jul 6;33(7):1483-1492.e10. DOI:10.1016/j.cmet.2021.04.009
4-IsoxazolecarboxaMide, 3-(2-chlorophenyl)-N-(4-chlorophenyl)-N,5-diMethyl- Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 33024 | 60 |
| career henan chemical co | +86-0371-86658258 +8613203830695 | sales@coreychem.com | China | 29859 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 32159 | 58 |
| HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 | sales@hzclap.com | CHINA | 6312 | 58 |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | sales@sarms4muscle.com | China | 10473 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6391 | 58 |
| ShenZhen Trendseen Biological Technology Co.,Ltd. | 13417589054 | trendseenbio@gmail.com | China | 11681 | 58 |
| Aladdin Scientific | tp@aladdinsci.com | United States | 57505 | 58 | |
| Amadis Chemical Company Limited | 571-89925085 | sales@amadischem.com | China | 131957 | 58 |
| Shanghai Boyle Chemical Co., Ltd. | sales@boylechem.com | China | 2922 | 55 |
View Lastest Price from 4-IsoxazolecarboxaMide, 3-(2-chlorophenyl)-N-(4-chlorophenyl)-N,5-diMethyl- manufacturers
| Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
|---|---|---|---|---|---|---|---|---|
 |
2024-11-19 | TGR5 Receptor Agonist
1197300-24-5
|
US $34.00-133.00 / mg | ≥95% | 10g | TargetMol Chemicals Inc. | ||
 |
2019-09-04 | 4-IsoxazolecarboxaMide, 3-(2-chlorophenyl)-N-(4-chlorophenyl)-N,5-diMethyl-
1197300-24-5
|
US $5.00 / KG | 1KG | 99% | 1ton | Career Henan Chemical Co |
-
- TGR5 Receptor Agonist
1197300-24-5
- US $34.00-133.00 / mg
- ≥95%
- TargetMol Chemicals Inc.
-
- 4-IsoxazolecarboxaMide, 3-(2-chlorophenyl)-N-(4-chlorophenyl)-N,5-diMethyl-
1197300-24-5
- US $5.00 / KG
- 99%
- Career Henan Chemical Co