J-2156 TFA is a high potent, selective somatostatin receptor type 4 (SST4 receptor) agonist with IC50s of 0.05 nM and 0.07 nM for human and rat SST4 receptors, respectively. J-2156 TFA has anti-inflammatory activity and it is used for the relief of mechanical allodynia and mechanical hyperalgesia in the ipsilateral hindpaws in rats.
| Molecular Weight | 582.59 |
| Formula | C26H29F3N4O6S |
| CAS Number | 2387505-73-7 |
| Form | Solid |
| Solubility (25°C) | Water 100 mg/mL (ultrasonic) DMSO 100 mg/mL (ultrasonic) |
| Storage | Store at ≤ -20°C, protect from light, dry, sealed |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related Somatostatin Receptor Products |
|---|
| TT-232
TT-232 (CAP-232), a somatostatin derivative, is a peptide SSTR1/SSTR4 agonist. |
| Cyclosomatostatin
Cyclosomatostatin is a potent somatostatin (SST) receptor antagonist. |
| Somatostatin-28 (1-14)
Somatostatin-28 (1-14) is an N-terminal fragment of the neuropeptide somatostatin-28. |
| CH 275
CH 275 is a peptide analog of somatostatin and binds preferably to somatostatin receptor 1 (sst1) with a Ki of 52 nM. |
| CYN 154806
CYN 154806, a cyclic octapeptide, is a potent and selective somatostatin sst2 receptor antagonist. |
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