Comparison

biie-0246

Item no. V2121-50mg
Manufacturer InvivoChem LLC
CASRN 246146-55-4
Amount 50mg
Category
Type Biochemicals
Specific against other
ECLASS 10.1 32160490
ECLASS 11.0 32160490
UNSPSC 12000000
Available
Description
InvivoChem Cat #:V2121CAS #:246146-55-4Purity >=98%

Description: BIIE0246, a newly synthesized, potent and highly selective non-peptide neuropeptide Y (NPY) Y2 receptor antagonist with an IC50 of 15 nM. It was able to compete with high affinity (8 to 15 nM) for specific (125)IPYY(3 - 36) binding sites in HEK293 cells transfected with the rat Y(2) receptor cDNA, and in rat brain and human frontal cortex membrane homogenates. Interestingly, in rat brain homogenates while NPY, C2-NPY and PYY(3 - 36) inhibited all specific (125)IPYY(3 - 36) labelling, BIIE0246 failed to compete for all specific binding suggesting that (125)IPYY(3 - 36) recognized, in addition to the Y(2) subtype, another population of specific NPY binding sites, most likely the Y(5) receptor. Quantitative receptor autoradiographic data confirmed the presence of (125)IPYY(3 - 36)/BIIE0246-sensitive (Y(2)) and-insensitive (Y(5)) binding sites in the rat brain as well as in the marmoset monkey and human hippocampal formation. In the rat vas deferens and dog saphenous vein (two prototypical Y(2) bioassays), BIIE0246 induced parallel shifts to the right of NPY concentration-response curves with pA(2) values of 8.1 and 8.6, respectively. In the rat colon (a Y(2)/Y(4) bioassay), BIIE0246 (1 microM) completely blocked the contraction induced by PYY(3 - 36), but not that of Leu(31), Pro(34)NPY (a Y(1), Y(4) and Y(5) agonist) and hPP (a Y(4) and Y(5) agonist). Additionally, BIIE0246 failed to alter the contractile effects of NPY in prototypical Y(1) in vitro bioassays. Taken together, these results demonstrate that BIIE0246 is a highly potent, high affinity antagonist selective for the Y(2) receptor subtype. It should prove most useful to establish further the functional role of the Y(2) receptor in the organism. europeptide Y (NPY) plays an important role in the regulation of energy homeostasis in the level of central and sympathetic nervous systems (SNSs).

References: Br J Pharmacol. 2000 Mar; 129(6):1075-88.; Front Pharmacol. 2018; 9: 319.


BIIE-0246

Name: BIIE-0246
CAS#: 246146-55-4
Chemical Formula: C49H57N11O6
Exact Mass: 895.44933
Molecular Weight: 896.05
Elemental Analysis: C, 65.68; H, 6.41; N, 17.19; O, 10.71
Storage
-20C for 3 years in powder form
-80C for 2 years in solvent
Technical Information
Synonym: AR-H 053591; AR H 053591; AR-H-053591; AR H053591; ARH053591; BIIE-0246; BIIE 0246; BIIE-0246; CHEMBL540989; GTPL1547; CTK8E9439; BIIE0246;
Chemical Name: (2S)-5-(diaminomethylideneamino)-N-[2-(3, 5-dioxo-1, 2-diphenyl-1, 2, 4-triazolidin-4-yl)ethyl]-2-[[2-[1-[2-oxo-2-[4-(6-oxo-5, 11-dihydrobenzo[c][1]benzazepin-11-yl)piperazin-1-yl]ethyl]cyclopentyl]acetyl]amino]pentanamide
InChi Key: RSJAXPUYVJKAAA-JPGJPTAESA-N
InChi Code: InChI=1S/C49H57N11O6/c50-46(51)53-25-13-22-40(45(64)52-26-27-58-47(65)59(34-14-3-1-4-15-34)60(48(58)66)35-16-5-2-6-17-35)54-41(61)32-49(23-11-12-24-49)33-42(62)56-28-30-57(31-29-56)43-36-18-7-8-19-37(36)44(63)55-39-21-10-9-20-38(39)43/h1-10, 14-21, 40, 43H, 11-13, 22-33H2, (H, 52, 64)(H, 54, 61)(H, 55, 63)(H4, 50, 51, 53)/t40-, 43?/m0/s1
SMILES Code: O=C(NCCN1C(N(C2=CC=CC=C2)N(C3=CC=CC=C3)C1=O)=O)[CH](NC(CC4(CC(N5CCN(C6C7=CC=CC=C7C(NC8=CC=CC=C68)=O)CC5)=O)CCCC4)=O)CCC/N=C(N)\N

Note: The presented information and documents (Manual, Product Datasheet, Safety Datasheet and Certificate of Analysis) correspond to our latest update and should serve for orientational purpose only. We do not guarantee the topicality. We would kindly ask you to make a request for specific requirements, if necessary.

All products are intended for research use only (RUO). Not for human, veterinary or therapeutic use.

Amount: 50mg
Available: In stock
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