SBI 810 HCl salt form · hydrochloride · Parent SBI-810 · Synonyms: SBI 810 hydorchloride
SBI-810 hydrochloride is a functionally selected β-arrestin-biased neurotensin receptor 1 allosteric modulator.
For research use only. Not for human or veterinary use.
SBI 810 HCl structure
CAS No.: 2772746-58-2
Pack sizes & pricing
| Size | Price | SKU | Stock | |
|---|---|---|---|---|
| 25 mg | USD 470.00 | BP-01161A-25mg | In stock | Get quote |
| 50 mg | USD 750.00 | BP-01161A-50mg | In stock | Get quote |
| 100 mg | USD 1,180.00 | BP-01161A-100mg | In stock | Get quote |
| 250 mg | USD 2,350.00 | BP-01161A-250mg | In stock | Get quote |
| 500 mg | USD 3,800.00 | BP-01161A-500mg | In stock | Get quote |
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Description
SBI-810 hydrochloride is a functionally selected β-arrestin-biased neurotensin receptor 1 (NTSR1) allosteric modulator. SBI-810 hydrochloride modulates NTSR1 G protein signaling in a G protein-specific manner in the presence of the endogenous ligand, neurotensin (NT). SBI-810 hydrochloride fully antagonizes NT-induced activation of Gq, partially antagonizes NT-induced activation of Gi1 and is permissive of NTSR1 activation of GoA and G12.
Biological activity
In Vitro SBI-810 (10 min) hydrochloride stimulates the recruitment of β-arrestin 2 to human NTSR1 in HEK293T cells, and antagonizes Gq activation induced by Neurotensin (NT) (HY-P0234). Bath-applied SBI-810 (5 μM, administered during recording) hydrochloride decreases the action potential firing frequency of DRG neurons, increases their rheobase, and inhibits neuronal excitability. In Vivo SBI-810 (12 mg/kg/10 µg~22 nmol); 1 µg; i.p./i.t.; single dose) hydrochloride exerts potent, NTSR1- and βarr2-dependent spinal analgesic effects in naive C57BL/6J mice, and alleviates physiological acute mechanical and thermal pain. SBI-810 (20 µg; i.t.; single dose) hydrochloride exerts potent analgesic effects on physiological acute mechanical pain in naive Sprague Dawley rats. SBI-810 (12 mg/kg; i.p.; single dose) hydrochloride potently inhibits pain in mouse plantar incision and tibial fracture post-surgical pain models. SBI-810 (12 mg/kg/10 µg; i.p./i.t.; single dose, administered 7 days post-surgery) hydrochloride exerts potent, NTSR1- and βarr2-dependent analgesic effects in SNI model mice, alleviating neuropathic mechanical allodynia and cold allodynia. SBI-810 (12 mg/kg; i.p.; single dose; administered concurrently with formalin injection) hydrochloride potently inhibits inflammatory hyperalgesia and mechanical allodynia, and reduces formalin-induced activation of nociceptors in DRG neurons in mouse formalin/CFA (HY-153808) inflammatory pain models. SBI-810 (12 mg/kg; i.p.; single dose; administered post-STZ-induced hyperglycemia) hydrochloride potently alleviates mechanical pain and cold pain in mice with STZ (HY-13753)-induced diabetic neuropathic pain. SBI-810 (12-30 mg/kg; i.p.; single dose) hydrochloride attenuates or abolishes morphine-induced CPP, and significantly reduces the cumulative withdrawal score induced by Naloxone (HY-17417A) in mice treated with escalating doses of morphine.
Identifiers
- SMILES
-
Cl.OCCN(C=1C=CC=2N=C(N=C(C2C1)N3CCC(C=4C=CC=CC4OC)CC3)C5(C)CC5)C - InChIKey
-
SZPSBVPAWFJWAL-UHFFFAOYSA-N
Specifications
- MW (average)
- 483.0450
- Formula
- C27H35ClN4O2
- CAS No.
- 2772746-58-2
- Physical state
- Solid
- Color
- light yellow to yellow
- Shipping
- Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
- Storage
- Powder 4℃ 2 years; In solvent -20℃ 1 month;
Solubility
soluble in DMSO