Product Name :
ARC 239 dihydrochloride
Description:
ARC 239 dihydrochloride is a selective antagonist of α2B adrenoceptor with pKD value of 8.8 . α2B adrenoceptor is a G-protein coupled receptor. α2-adrenergic receptors include three subtypes: α2A, α2B and α2C, which play an important role in regulating neurotransmitter release from adrenergic neurons in the central nervous system and from sympathetic nerves. ARC 239 dihydrochloride is a selective α2B adrenoceptor antagonist. In rat brain, ARC 239 inhibited the binding of 5-HTIA receptor radioligands 8-OH-DPAT and RX 821002 to cortical membranes with Ki values of 63.1 and 136 nM respectively, which suggested that ARC 239 recognized 5-HT1A receptor . Treatment human platelets with ARC 239 significantly inhibited platelet aggregation induced by adenosine diphosphate (ADP), epinephrine and arachidonic acid and increased collagen/epinephrine closure time, which suggested that α2B adrenoceptor play a critical role in platelet aggregation . In cervical samples isolated from pregnant rats, ARC 239 effectively inhibited noradrenaline-stimulated contractions . In C57BL/6 mice with gastric mucosal damage induced by acidified ethanol, ARC 239 (10.4 nM) antagonized gastroprotective effect induced by α2-adrenoceptor agonists .
CAS:
55974-42-0
Molecular Weight:
480.43
Formula:
C24H31Cl2N3O3
Chemical Name:
2-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-4,4-dimethyl-1,2,3,4-tetrahydroisoquinoline-1,3-dione dihydrochloride
Smiles :
Cl.Cl.CC1(C)C2=CC=CC=C2C(=O)N(CCN2CCN(CC2)C2=CC=CC=C2OC)C1=O
InChiKey:
SAJKHRHHDGSJEZ-UHFFFAOYSA-N
InChi :
InChI=1S/C24H29N3O3.2ClH/c1-24(2)19-9-5-4-8-18(19)22(28)27(23(24)29)17-14-25-12-15-26(16-13-25)20-10-6-7-11-21(20)30-3;;/h4-11H,12-17H2,1-3H3;2*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:
ARC 239 dihydrochloride is a selective antagonist of α2B adrenoceptor with pKD value of 8.8 . α2B adrenoceptor is a G-protein coupled receptor. α2-adrenergic receptors include three subtypes: α2A, α2B and α2C, which play an important role in regulating neurotransmitter release from adrenergic neurons in the central nervous system and from sympathetic nerves. ARC 239 dihydrochloride is a selective α2B adrenoceptor antagonist.{{Ravuconazole} web|{Ravuconazole} Inhibitor|{Ravuconazole} Immunology/Inflammation|{Ravuconazole} Protocol|{Ravuconazole} In Vivo|{Ravuconazole} manufacturer} In rat brain, ARC 239 inhibited the binding of 5-HTIA receptor radioligands 8-OH-DPAT and RX 821002 to cortical membranes with Ki values of 63.{{Carnosol} MedChemExpress|{Carnosol} Keap1-Nrf2|{Carnosol} Biological Activity|{Carnosol} In Vivo|{Carnosol} supplier|{Carnosol} Autophagy} 1 and 136 nM respectively, which suggested that ARC 239 recognized 5-HT1A receptor . Treatment human platelets with ARC 239 significantly inhibited platelet aggregation induced by adenosine diphosphate (ADP), epinephrine and arachidonic acid and increased collagen/epinephrine closure time, which suggested that α2B adrenoceptor play a critical role in platelet aggregation . In cervical samples isolated from pregnant rats, ARC 239 effectively inhibited noradrenaline-stimulated contractions . In C57BL/6 mice with gastric mucosal damage induced by acidified ethanol, ARC 239 (10.4 nM) antagonized gastroprotective effect induced by α2-adrenoceptor agonists .PMID:24456950 |Product information|CAS Number: 55974-42-0|Molecular Weight: 480.43|Formula: C24H31Cl2N3O3|Chemical Name: 2-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-4,4-dimethyl-1,2,3,4-tetrahydroisoquinoline-1,3-dione dihydrochloride|Smiles: Cl.Cl.CC1(C)C2=CC=CC=C2C(=O)N(CCN2CCN(CC2)C2=CC=CC=C2OC)C1=O|InChiKey: SAJKHRHHDGSJEZ-UHFFFAOYSA-N|InChi: InChI=1S/C24H29N3O3.2ClH/c1-24(2)19-9-5-4-8-18(19)22(28)27(23(24)29)17-14-25-12-15-26(16-13-25)20-10-6-7-11-21(20)30-3;;/h4-11H,12-17H2,1-3H3;2*1H|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.|
