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MedKoo Cat#: 524418 | Name: BIIE-0246 HCl
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

BIIE-0246 is a potent, selective and competitive non-peptide antagonist for the neuropeptide Y Y2 receptor. BIIE-0246 displays > 650-fold selectivity over Y1, Y4 and Y5 receptors.

Chemical Structure

BIIE-0246 HCl
BIIE-0246 HCl
CAS#246146-31-6 (2HCl)

Theoretical Analysis

MedKoo Cat#: 524418

Name: BIIE-0246 HCl

CAS#: 246146-31-6 (2HCl)

Chemical Formula: C49H59Cl2N11O6

Exact Mass: 895.4493

Molecular Weight: 968.98

Elemental Analysis: C, 60.74; H, 6.14; Cl, 7.32; N, 15.90; O, 9.91

Price and Availability

Size Price Availability Quantity
5mg USD 450.00 2 Weeks
25mg USD 1,250.00 2 Weeks
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Related CAS #
246146-31-6 (2HCl) 246146-55-4 (free base) 2624332-04-1 (HCl)
Synonym
BIIE-0246 HCl; BIIE 0246 HCl; BIIE0246 HCl; CHEMBL540989; GTPL1547; CTK8E9439; AR-H 053591 hydrochloride; AR-H 053591 HCl; AR-H053591 HCl;
IUPAC/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 dihydrochloride
InChi Key
UESZCTPNTRZXHQ-SICTUBFJSA-N
InChi Code
InChI=1S/C49H57N11O6.2ClH/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);2*1H/t40-,43?;;/m0../s1
SMILES Code
O=C(NCCN1C(N(C2=CC=CC=C2)N(C3=CC=CC=C3)C1=O)=O)[C@@H](NC(CC4(CC(N5CCN(C6C7=CC=CC=C7C(NC8=CC=CC=C68)=O)CC5)=O)CCCC4)=O)CCC/N=C(N)\N.[H]Cl.[H]Cl
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
BIIE-0246 is a potent and highly selective non-peptide neuropeptide Y (NPY) Y2 receptor antagonist, with an IC50 of 15 nM.
In vitro activity:
BIIE0246 significantly antagonized the effects of NPY and of [ahx5-24]NPY. For example, in the presence of 30 nm BIIE0246, the inhibition caused by 1 μm NPY was reduced to about 40% of its control values. Interestingly, the antagonism of the action of NPY by BIIE0246 appeared to depend on the concentration of the agonist, and was greater at higher agonist concentrations. Similarly, the antagonism by BIIE0246 of most concentrations of [ahx5-24]NPY was more effective at greater agonist concentrations. Reference: Br J Pharmacol. 2002 Jun; 136(4): 502–509. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1573380/
In vivo activity:
Specific Y2-receptor antagonist, BIIE0246, was administered (1.3 mg/kg/day, i.p.) for 2 or 4.5 weeks to OE-NPYDβH and WT mice feeding on chow or Western diet. Treatment with Y2-receptor antagonist increased body weight gain in both genotypes on chow diet and caused metabolic disturbances (e.g., hyperinsulinemia and hypercholesterolemia), especially in WT mice. During energy surplus (i.e., on Western diet), blocking of Y2-receptors induced obesity in WT mice, whereas OE-NPYDβH mice showed reduced fat mass gain, hepatic glycogen and serum cholesterol levels relative to body adiposity. Reference: Front Pharmacol. 2018 Apr 5;9:319. https://pubmed.ncbi.nlm.nih.gov/29674968/
Solvent mg/mL mM comments
Solubility
DMSO 100.0 111.60
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 968.98 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. El Bahh B, Cao JQ, Beck-Sickinger AG, Colmers WF. Blockade of neuropeptide Y(2) receptors and suppression of NPY's anti-epileptic actions in the rat hippocampal slice by BIIE0246. Br J Pharmacol. 2002 Jun;136(4):502-9. doi: 10.1038/sj.bjp.0704751. PMID: 12055128; PMCID: PMC1573380. 2. Weiser T, Wieland HA, Doods HN. Effects of the neuropeptide Y Y(2) receptor antagonist BIIE0246 on presynaptic inhibition by neuropeptide Y in rat hippocampal slices. Eur J Pharmacol. 2000 Sep 15;404(1-2):133-6. doi: 10.1016/s0014-2999(00)00478-7. PMID: 10980271. 3. Ailanen L, Vähätalo LH, Salomäki-Myftari H, Mäkelä S, Orpana W, Ruohonen ST, Savontaus E. Peripherally Administered Y2-Receptor Antagonist BIIE0246 Prevents Diet-Induced Obesity in Mice With Excess Neuropeptide Y, but Enhances Obesity in Control Mice. Front Pharmacol. 2018 Apr 5;9:319. doi: 10.3389/fphar.2018.00319. PMID: 29674968; PMCID: PMC5895854. 4. Bacchi F, Mathé AA, Jiménez P, Stasi L, Arban R, Gerrard P, Caberlotto L. Anxiolytic-like effect of the selective neuropeptide Y Y2 receptor antagonist BIIE0246 in the elevated plus-maze. Peptides. 2006 Dec;27(12):3202-7. doi: 10.1016/j.peptides.2006.07.020. Epub 2006 Sep 7. PMID: 16959374.
In vitro protocol:
1. El Bahh B, Cao JQ, Beck-Sickinger AG, Colmers WF. Blockade of neuropeptide Y(2) receptors and suppression of NPY's anti-epileptic actions in the rat hippocampal slice by BIIE0246. Br J Pharmacol. 2002 Jun;136(4):502-9. doi: 10.1038/sj.bjp.0704751. PMID: 12055128; PMCID: PMC1573380. 2. Weiser T, Wieland HA, Doods HN. Effects of the neuropeptide Y Y(2) receptor antagonist BIIE0246 on presynaptic inhibition by neuropeptide Y in rat hippocampal slices. Eur J Pharmacol. 2000 Sep 15;404(1-2):133-6. doi: 10.1016/s0014-2999(00)00478-7. PMID: 10980271.
In vivo protocol:
1. Ailanen L, Vähätalo LH, Salomäki-Myftari H, Mäkelä S, Orpana W, Ruohonen ST, Savontaus E. Peripherally Administered Y2-Receptor Antagonist BIIE0246 Prevents Diet-Induced Obesity in Mice With Excess Neuropeptide Y, but Enhances Obesity in Control Mice. Front Pharmacol. 2018 Apr 5;9:319. doi: 10.3389/fphar.2018.00319. PMID: 29674968; PMCID: PMC5895854. 2. Bacchi F, Mathé AA, Jiménez P, Stasi L, Arban R, Gerrard P, Caberlotto L. Anxiolytic-like effect of the selective neuropeptide Y Y2 receptor antagonist BIIE0246 in the elevated plus-maze. Peptides. 2006 Dec;27(12):3202-7. doi: 10.1016/j.peptides.2006.07.020. Epub 2006 Sep 7. PMID: 16959374.
1: Yang XP, Chiba S. Antagonistic interaction between BIIE 0246, a neuropeptide Y Y2-receptor antagonist, and omega-conotoxin GVIA, a Ca2+ channel antagonist, in presynaptic transmitter releases in dog splenic arteries. Jpn J Pharmacol. 2002 Jun;89(2):188-91. PubMed PMID: 12120763.