Product Name :
BW 373U86
Description:
Ki: 1.8, 15, 85 and 34 nM for delta, mu, epsilon and kappa receptor Opioid receptors are heterogeneous and at least four types, mu,.delta, kappa and epsilon, are known to exist. Currently, all clinically used opiates act through the mu receptor to induce analgesia; however, they also induce unwanted side effects such as respiratory depression, dependence, constipation and muscle rigidity.BW 373U86 is a novel, potent and selective nonpeptidic delta opioid receptor agonist. In vitro: BW 373U86 was a potent delta receptor-selective ligand in receptor binding assays. The Ki values were 1 .8 ± 0.4, 15 ± 3, 85 ± 4 and 34 ± 3 nM for delta, mu, epsilon and kappa receptor binding sites, respectively. BW 373U86 inhibited electncally evoked muscle contraction of mouse vas deferens with an ED50 value of 0.2 ± 0.06 nM . In vivo: BW 373U86 inhibited the acoustic startle reflex after subcutaneous administration from 0.2- to 2-mg/kg doses in rats, and this inhibition was blocked by naltnndole. BW 373U86 also induced a dose-dependent increase of locomotor activity in rats at similar doses. This effect was inhibited by naltnndole . Clinical trial: Up to now, BW 373U86 is still in the preclinical development stage.
CAS:
155836-50-3
Molecular Weight:
435.60
Formula:
C27H37N3O2
Chemical Name:
4-[(R)-[(2S,5R)-2,5-dimethyl-4-(prop-2-en-1-yl)piperazin-1-yl](3-hydroxyphenyl)methyl]-N,N-diethylbenzamide
Smiles :
C[C@H]1CN(CC=C)[C@H](C)CN1[C@@H](C1C=C(O)C=CC=1)C1C=CC(=CC=1)C(=O)N(CC)CC
InChiKey:
LBLDMHBSVIVJPM-YZIHRLCOSA-N
InChi :
InChI=1S/C27H37N3O2/c1-6-16-29-18-21(5)30(19-20(29)4)26(24-10-9-11-25(31)17-24)22-12-14-23(15-13-22)27(32)28(7-2)8-3/h6,9-15,17,20-21,26,31H,1,7-8,16,18-19H2,2-5H3/t20-,21+,26-/m1/s1
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:
Ki: 1.8, 15, 85 and 34 nM for delta, mu, epsilon and kappa receptor Opioid receptors are heterogeneous and at least four types, mu,.delta, kappa and epsilon, are known to exist. Currently, all clinically used opiates act through the mu receptor to induce analgesia; however, they also induce unwanted side effects such as respiratory depression, dependence, constipation and muscle rigidity.BW 373U86 is a novel, potent and selective nonpeptidic delta opioid receptor agonist. In vitro: BW 373U86 was a potent delta receptor-selective ligand in receptor binding assays. The Ki values were 1 .8 ± 0.4, 15 ± 3, 85 ± 4 and 34 ± 3 nM for delta, mu, epsilon and kappa receptor binding sites, respectively. BW 373U86 inhibited electncally evoked muscle contraction of mouse vas deferens with an ED50 value of 0.2 ± 0.06 nM . In vivo: BW 373U86 inhibited the acoustic startle reflex after subcutaneous administration from 0.{{Amlodipine} medchemexpress|{Amlodipine} Calcium Channel|{Amlodipine} Technical Information|{Amlodipine} Data Sheet|{Amlodipine} custom synthesis|{Amlodipine} Cancer} 2- to 2-mg/kg doses in rats, and this inhibition was blocked by naltnndole.{{Solanezumab} MedChemExpress|{Solanezumab} Neuronal Signaling|{Solanezumab} Technical Information|{Solanezumab} Data Sheet|{Solanezumab} supplier|{Solanezumab} Epigenetic Reader Domain} BW 373U86 also induced a dose-dependent increase of locomotor activity in rats at similar doses.PMID:24456950 This effect was inhibited by naltnndole . Clinical trial: Up to now, BW 373U86 is still in the preclinical development stage.|Product information|CAS Number: 155836-50-3|Molecular Weight: 435.60|Formula: C27H37N3O2|Chemical Name: 4-[(R)-[(2S,5R)-2,5-dimethyl-4-(prop-2-en-1-yl)piperazin-1-yl](3-hydroxyphenyl)methyl]-N,N-diethylbenzamide|Smiles: C[C@H]1CN(CC=C)[C@H](C)CN1[C@@H](C1C=C(O)C=CC=1)C1C=CC(=CC=1)C(=O)N(CC)CC|InChiKey: LBLDMHBSVIVJPM-YZIHRLCOSA-N|InChi: InChI=1S/C27H37N3O2/c1-6-16-29-18-21(5)30(19-20(29)4)26(24-10-9-11-25(31)17-24)22-12-14-23(15-13-22)27(32)28(7-2)8-3/h6,9-15,17,20-21,26,31H,1,7-8,16,18-19H2,2-5H3/t20-,21+,26-/m1/s1|Technical Data|Appearance: Solid Power|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.|Drug Formulation: To be determined|HS Tariff Code: 382200|Products are for research use only. Not for human use.|
