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[CAS NO. 1620992-67-7] GPR81agonist1
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-135982 |
| Brand: | MCE |
| CAS: | 1620992-67-7 |
Overview
| MDL | - |
|---|---|
| Molecular Weight | 446.63 |
| Molecular Formula | C22H30N4O2S2 |
| SMILES | O=C([C@H]1CC[C@H](C)CC1)NC2=NC(C3=CC=CS3)=C(CC(N4CCN(C)CC4)=O)S2 |
Summary
GPR81 agonist 1 is a potent and highly selective GPR81 agonist, with EC 50 s of 58 nM and 50 nM for human and mouse GPR81, respectively. GPR81 agonist 1 inhibits lipolysis in differentiated 3T3-L1 adipocytes. GPR81 agonist 1 suppresses lipolysis in mice without cutaneous flushing. GPR81 agonist 1 displays remarkable selectivity for GPR81 over GPR109a [1] .
In Vitro
GPR81 agonist 1 (compound 2) (1-1000 nM) inhibits lipolysis in differentiated 3T3-L1 adipocytes [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
GPR81 agonist 1 (100 mg/kg; i.p.) suppresses lipolysis in mice without cutaneous flushing
[1]
.
GPR81 agonist 1 (10 mg/kg; i.p.) shows good bioavailability (71%) and C
max
(6.3 μM)
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Nine-week-old male C57/Bl6 mice (fed and fasted mice) [1] |
| Dosage: | 100 mg/kg |
| Administration: | I.p. |
| Result: | Reduced plasma FFA content of fed and fasted mice by approximately 50% and 35%, respectively, at 15 min postdose when intraperitoneally administered at a dose of 100 mg/kg. |
| Animal Model: | Male C57/Bl6 mice [1] |
| Dosage: | 10 mg/kg (Pharmacokinetic Analysis) |
| Administration: | I.p.(Pharmacokinetic Analysis) |
| Result: | Showed good bioavailability (71%) and C max (6.3 μM). |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 50 mg/mL ( 111.95 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.2390 mL | 11.1949 mL | 22.3899 mL |
| 5 mM | 0.4478 mL | 2.2390 mL | 4.4780 mL |
| 10 mM | 0.2239 mL | 1.1195 mL | 2.2390 mL |
-
1.
-
2.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (5.60 mM); Clear solution
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