AR 231453 |
| Katalog-Nr.GC14944 |
AR 231453 ist ein potenter, spezifischer und oral verfÜgbarer GPR119-Agonist.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 733750-99-7
Sample solution is provided at 25 µL, 10mM.
;)
_1-7.$$$37316672@70.jpg');)
;)
;)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
;)
;)
;)
_1124-1138.$$$35908550@30.jpg');)
_766-780.$$$37100057@30.jpg');)
_418-432.$$$36893736@30.jpg');)
_240-255.$$$35108512@29.jpg');)
_533-545.$$$36543525@28.jpg');)
_264-276.$$$36600053@22.jpg');)
_2214998.$$$@0.jpg');)
AR 231453 is an agonist of GPR119 with EC50 value of 0.68nM [1].
AR 231453 is the first subnanomolar agonist of GPR119. It is highly selective against GPR119 over a 76 receptor and enzyme profiling panel (CEREP) including the known incretin receptors. It also has no activity to 140 known and orphan GPCRs in melanophore dispersion assays. Besides that, AR 231453 is reported to stimulate cAMP production via endogenously expressed GPR119 in HIT-T15 cell line with EC50 value of 4.7nM [1].
In vivo assay shows that AR 231453 has activity in rodents. It can enhance glucose-dependent insulin release and improve oral glucose tolerance in wild-type C57/bl6J mice but not in GPR119-deficient mice at a dose of 20 mg/kg. Due to its activity to active GPR119, AR 231453 is expected to be a potent anti-diabetic agent [1].
References:
[1] Semple G, Fioravanti B, Pereira G, Calderon I, Uy J, Choi K, Xiong Y, Ren A, Morgan M, Dave V, Thomsen W, Unett DJ, Xing C, Bossie S, Carroll C, Chu ZL, Grottick AJ, Hauser EK, Leonard J, Jones RM. Discovery of the first potent and orally efficacious agonist of the orphan G-protein coupled receptor 119. J Med Chem. 2008 Sep 11;51(17):5172-5.
| Cas No. | 733750-99-7 | SDF | |
| Chemical Name | N-(2-fluoro-4-methylsulfonylphenyl)-5-nitro-6-[4-(3-propan-2-yl-1,2,4-oxadiazol-5-yl)piperidin-1-yl]pyrimidin-4-amine | ||
| Canonical SMILES | CC(C)C1=NOC(=N1)C2CCN(CC2)C3=C(C(=NC=N3)NC4=C(C=C(C=C4)S(=O)(=O)C)F)[N+](=O)[O-] | ||
| Formula | C21H24FN7O5S | M.Wt | 505.52 |
| Löslichkeit | ≥ 49.3 mg/mL in DMSO with gentle warming | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.9782 mL | 9.8908 mL | 19.7816 mL |
| 5 mM | 0.3956 mL | 1.9782 mL | 3.9563 mL |
| 10 mM | 0.1978 mL | 0.9891 mL | 1.9782 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 19 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *