BRL-15572(BRL15572)|h5-HT1D inhibitor|DC Chemicals

Cas No.:	1173022-77-9
Chemical Name:	3-(4-(3-chlorophenyl)piperazin-1-yl)-1,1-diphenylpropan-2-oldihydrochloride
Synonyms:	BRL-15572; BRL15572 ; BRL 15572 dihydrochloride; BRL15572 dihydrochloride
SMILES:	OC(CN1CCN(C2=CC(Cl)=CC=C2)CC1)C(C3=CC=CC=C3)C4=CC=CC=C4.[H]Cl
Formula:	C₂₅H₂₇ClN₂O^.₂HCl
M.Wt:	479.87
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

BRL-15572 displays high affinity and selectivity For h5-HT1D receptors. BRL-15572 has 60-fold higher affinity For h5-HT1D than 5-HT1B receptors. BRL-15572 binds to h5-HT1B and h5-HT1D receptors with pKB of less than 6 and 7.1, respectively. BRL-15572 stimulates [35S]GTP γ S binding in both cell lines, with potencies that correlated with their receptor binding affinities in both h5-HT1B and h5-HT1D receptor expressing cell lines. BRL-15572 reveals receptor binding affinities For 5-HT1A, 5-HT1B, 5-HT1E, 5-HT1F, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT6 and 5-HT7 with pKi of 7.7, 6.1, 5.2, 6.0, 6.6, 7.4, 6.2, 5.9 and 6.3, respectively. In the h5-HT1D cell line, both BRL-15572 (1 µM) shifts the 5-HT concentration response curve with pKB of 7.1, respectively. BRL-15572 does have moderately high affinity at human 5-HT1A and 5-HT2B receptors. In human atrial appendages, the electrically evoked tritium overflow is inhibited by 5-HT in a manner susceptible to antagonism by BRL-15572 (300 nM; 23 times Ki at h5-HT1D receptors). The inhibitory effect of 5-HT on the K+-evoked overflow of glutamate is antagonized by the h5-HT1D receptor ligand BRL-15572. BRL-15572 (1 μM) is unable to modify the effect of 5-HT at the autoreceptor regulating [3H]5-HT release. The selective 5-HT1D/1B receptor antagonist BRL 15572 inhibits the effect of the agonist L-694 247. For the detailed information of BRL-15572 dihydrochloride, the solubility of BRL-15572 dihydrochloride in water, the solubility of BRL-15572 dihydrochloride in DMSO, the solubility of BRL-15572 dihydrochloride in PBS buffer, the animal experiment (test) of BRL-15572 dihydrochloride, the cell expriment (test) of BRL-15572 dihydrochloride, the in vivo, in vitro and clinical trial test of BRL-15572 dihydrochloride, the EC50, IC50,and Affinity of BRL-15572 dihydrochloride, Please contact DC Chemicals.

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101

Cat. No.	Product name	Field of application
DC47777	FPPQ	FPPQ is a dual-acting 5-HT3 (Ki = 0.9 nM) and 5-HT6 (Ki = 3 nM) receptor antagonist with antipsychotic and procognitive properties.
DC47056	Usmarapride	Usmarapride (SUVN-D4010) is a selective 5-HT4 receptor ligand with EC50 value 27.5nM, intended for the symptomatic research of Alzheimer's disease and other disorders of memory and cognition like attention deficient hyperactivity, Parkinson's and schizophrenia.
DC46838	SB 258719 hydrochloride	SB 258719 (hydrochloride) is a selective 5-HT7 receptor antagonist displayed high affnity (pKi=7.5) for the receptor. SB-258719 (hydrochloride) shows apparent partial inverse agonism.
DC46837	Felcisetrag	Felcisetrag (TD-8954) is an orally active, potent and selective 5-HT4 receptor agonist with gastrointestinal prokinetic properties. Felcisetrag has high affinity (pKi =9.4) for human 5-HT4(c) receptors.
DC46498	SB-221284	SB 221284 is a selective 5-HT2C/2B receptor antagonist with pKi values are 6.4, 7.9 and 8.6 for 5-HT2A, 5-HT2B and 5-HT2C receptors, respectively. SB 221284 can be used for the research of neurological disease.
DC46478	DR4485 hydrochloride	DR4485 (hydrochloride) is an orally active and selective 5-HT7 antagonist (pKi=8.14).
DC46462	Renzapride	Renzapride (BRL 24924), a substituted benzamide, is a full 5-HT4 receptor agonist with a Ki value of 115 nM. Renzapride (BRL 24924) is also a 5HT2b and 5HT3 receptor antagonist. Renzapride could be used for constipation predominant irritable bowel syndrome (C-IBS) study.
DC46454	NAS181	NAS181 is a potent and selective antagonist of rat 5-HT1B receptor, with a Ki of 47 nM. NAS181 shows 13-fold selectivity for r5-HT1B over bovine 5-HT1B receptor (Ki=630 nM). NAS181 increases the 5-HT turnover and the synaptic concentration of 5-HT by inhibiting terminal r5-HT1B autoreceptors.
DC46452	WAY-100135 dihydrochloride	WAY-100135 dihydrochloride is a selective antagonist at presynaptic and postsynaptic 5-HT1A receptor, with an IC50 of 34 nM at the rat hippocampal 5-HT1A receptor. WAY-100135 dihydrochloride has potential antipsychotic properties.
DC46291	Org37684	Org37684 is a highly potent 5-HT2C receptor agonist (pEC50=8.17). Org37684 exhibits a rank order of potency of 5-HT2C>5-HT2B>5-HT2A. Its selectivity for the 5-HT2C receptor is approximately 2.5 times over the 5-HT2B (pEC50=7.96) and ten times for the 5-HT2A (pEC50=7.11) receptor.