Product Name :
SB-224289 hydrochloride
Description:
SB-224289 hydrochloride is a selective 5-HT1B receptor antagonist, with anxiolytic effect.
CAS:
180084-26-8
Molecular Weight:
557.08
Formula:
C32H33ClN4O3
Chemical Name:
1′-methyl-5-[2′-methyl-4′-(5-methyl-1,2,4-oxadiazol-3-yl)-[1,1′-biphenyl]-4-carbonyl]-2,5,6,7-tetrahydrospiro[furo[2,3-f]indole-3,4′-piperidine] hydrochloride
Smiles :
Cl.CN1CCC2(COC3=CC4CCN(C(=O)C5C=CC(=CC=5)C5=CC=C(C=C5C)C5N=C(C)ON=5)C=4C=C23)CC1
InChiKey:
GKGKBZYMDILCOF-UHFFFAOYSA-N
InChi :
InChI=1S/C32H32N4O3.ClH/c1-20-16-25(30-33-21(2)39-34-30)8-9-26(20)22-4-6-23(7-5-22)31(37)36-13-10-24-17-29-27(18-28(24)36)32(19-38-29)11-14-35(3)15-12-32;/h4-9,16-18H,10-15,19H2,1-3H3;1H
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
SB-224289 hydrochloride is a selective 5-HT1B receptor antagonist, with anxiolytic effect.|Product information|CAS Number: 180084-26-8|Molecular Weight: 557.08|Formula: C32H33ClN4O3|Chemical Name: 1′-methyl-5-[2′-methyl-4′-(5-methyl-1,2,4-oxadiazol-3-yl)-[1,1′-biphenyl]-4-carbonyl]-2,5,6,7-tetrahydrospiro[furo[2,3-f]indole-3,4′-piperidine] hydrochloride|Smiles: Cl.CN1CCC2(COC3=CC4CCN(C(=O)C5C=CC(=CC=5)C5=CC=C(C=C5C)C5N=C(C)ON=5)C=4C=C23)CC1|InChiKey: GKGKBZYMDILCOF-UHFFFAOYSA-N|InChi: InChI=1S/C32H32N4O3.ClH/c1-20-16-25(30-33-21(2)39-34-30)8-9-26(20)22-4-6-23(7-5-22)31(37)36-13-10-24-17-29-27(18-28(24)36)32(19-38-29)11-14-35(3)15-12-32;/h4-9,16-18H,10-15,19H2,1-3H3;1H|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO : 14.29 mg/mL (25.65 mM; Need ultrasonic). H2O : Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|In Vitro:|SB-224289 has specific toxin-blocking ability and does not inhibit Cho1p. SB-224289 (100 μM-25 μM) shows consistent efficacy at producing Pap-A resistance. SB-224289 does not directly inhibit the PS synthase enzyme in this in vitro assay. Moreover, SB-224289 specifically blocks the activity of papuamides and not other membrane disruptors. SB-224289 is unable to protect wild-type cells against KF, but it is able to provide protection against TPap-A. SB-224289 has a pKi of 8 at human cloned 5-HT1B receptors and displays more than 80 fold selectivity over the closely related 5-HT1D receptor and a range of other receptors. SB-224289 is a potent antagonist with pEC50 of 7.9±0.1. SB-224289 evokes a parallel rightward shift in the 5-HT concentration response curve with pA2 of 8.Protease Inhibitor Cocktail custom synthesis 4±0.Umbralisib Autophagy 2.PMID:33274953 SB-224289 (100 nM and 1 μM) also significantly increases [3H]-5HT release in electrically stimulated guinea-pig brain cortex slices.|In Vivo:|SB-224289 (SB 224289) alone or in combination with cocaine, increases anxiety-like behavior. SB 224289 significantly reduces the amount of locomotor activity in the cocaine-treated rats. SB 224289-treated animals spend a significantly longer time in the corners than those treated with vehicle. SB 224289 is a potent antagonist with an ED50 of 3.6 mg/kg, p.o in SK&F-99101-induced hypothermia in the guinea-pig. SB 224289 (4 mg/kg, p.o) reverses sumatriptan-induced inhibition of 5-HT release showing that it is also a potent terminal 5-HT autoreceptor antagonist in vivo. SB 224289 (2-16 mg/kg, p.o) does not increase 5-HT levels in the fuinea-pig frontal cortex. However, SB 224289 (4 mg/kg, p.o) causes a significantly increase in levels of 5-HT in the fuinea-pig dentate gyrus.|Products are for research use only. Not for human use.|
