BMS193885 lactate | CAS# 679839-66-8 | NPY Y1 receptor antagonist

MedKoo Cat#: 574340 | Name: BMS193885 lactate

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Description:

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

BMS-193885 is a potent, competitive neuropeptide (NPY) Y1 antagonist (Ki = 3.3 nM, IC50 = 5.9 nM) that displays > 47, > 100, > 160, > 160 and > 160-fold selectivity over σ1, α1, Y2, Y4 and Y5 receptors respectively. It reduces food intake and body weight via central Y1 inhibition and is brain penetrant. BMS-193885 has 3.3 nM affinity at the neuropeptide Y(1) receptor, acting competitively at the neuropeptide Y binding site. BMS-193885 increased the K(d) of [(125)I]PeptideYY from 0.35 nM to 0.65 nM without changing the B(max) (0.16 pmol/mg of protein) in SK-N-MC cells that endogenously express the neuropeptide Y(1) receptor. It is also found to be a full antagonist with an apparent K(b) of 4.5 nM measured by reversal of forskolin (FK)-stimulated inhibition of cAMP production by neuropeptide Y.

Chemical Structure

BMS193885 lactate

CAS#679839-66-8 (lactate)

Theoretical Analysis

MedKoo Cat#: 574340

Name: BMS193885 lactate

CAS#: 679839-66-8 (lactate)

Chemical Formula: C36H48N4O9

Exact Mass: 0.0000

Molecular Weight: 680.80

Elemental Analysis: C, 63.51; H, 7.11; N, 8.23; O, 21.15

Price and Availability

Size	Price	Availability	Quantity
10mg	USD 650.00	2 Weeks

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Related CAS #

186185-03-5 (free base) 186185-02-4 (HCl) 679839-66-8 (lactate)

Synonym

BMS193885 lactate; BMS-193885, BMS193885, BMS 193885;

IUPAC/Chemical Name

1,4-Dihydro-4-[3-[[[[3-[4-(3-methoxyphenyl)-1-piperidinyl]propyl]amino]carbonyl]amino]phenyl]-2,6-dimethyl-3,5-pyridinedicarboxylic acid 3,5-dimethyl ester L-Lactate

InChi Key

BYHJIPSVXAFCDI-WNQIDUERSA-N

InChi Code

InChI=1S/C33H42N4O6.C3H6O3/c1-21-28(31(38)42-4)30(29(22(2)35-21)32(39)43-5)25-10-6-11-26(19-25)36-33(40)34-15-8-16-37-17-13-23(14-18-37)24-9-7-12-27(20-24)41-3;1-2(4)3(5)6/h6-7,9-12,19-20,23,30,35H,8,13-18H2,1-5H3,(H2,34,36,40);2,4H,1H3,(H,5,6)

SMILES Code

CC1=C(C(OC)=O)C(C2=CC(NC(NCCCN3CCC(C4=CC=CC(OC)=C4)CC3)=O)=CC=C2)C(C(OC)=O)=C(C)N1.C[C@H](O)C(O)=O

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

Shelf Life

>3 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:

Potent, competitive NPY Y1 receptor antagonist.

In vitro activity:

TBD

In vivo activity:

Blockade of NPY Y(1) receptors with an intravenous dose of 5 mg/kg of BMS 193885, reduced significantly the cardio-respiratory effects of NPY injection in rats. Reference: Pharmacol Res. 2010 Nov;62(5):444-9. https://pubmed.ncbi.nlm.nih.gov/20600918/

	Solvent	mg/mL	mM
Solubility
	DMSO	68.1	100.00
	Water	13.6	20.00

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 680.80 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.

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. Kaczyńska K, Szereda-Przestaszewska M. NPY Y(1) receptors are involved in cardio-respiratory responses to intravenous injection of neuropeptide Y in anaesthetized rats. Pharmacol Res. 2010 Nov;62(5):444-9. doi: 10.1016/j.phrs.2010.06.006. Epub 2010 Jun 17. PMID: 20600918. 2. Antal-Zimanyi I, Bruce MA, Leboulluec KL, Iben LG, Mattson GK, McGovern RT, Hogan JB, Leahy CL, Flowers SC, Stanley JA, Ortiz AA, Poindexter GS. Pharmacological characterization and appetite suppressive properties of BMS-193885, a novel and selective neuropeptide Y(1) receptor antagonist. Eur J Pharmacol. 2008 Aug 20;590(1-3):224-32. doi: 10.1016/j.ejphar.2008.06.032. Epub 2008 Jun 12. PMID: 18573246.

In vitro protocol:

TBD

In vivo protocol:

1: Sakai K, Sanders KM, Lin SH, Pavlenko D, Funahashi H, Lozada T, Hao S, Chen CC, Akiyama T. Low-Threshold Mechanosensitive VGLUT3-Lineage Sensory Neurons Mediate Spinal Inhibition of Itch by Touch. J Neurosci. 2020 Sep 30;40(40):7688-7701. doi: 10.1523/JNEUROSCI.0091-20.2020. Epub 2020 Sep 7. PMID: 32895292; PMCID: PMC7531552. 2: Kawamura K, Mori W, Fujinaga M, Yamasaki T, Zhang Y, Wakizaka H, Hatori A, Xie L, Kumata K, Ohkubo T, Kurihara Y, Ogawa M, Nengaki N, Zhang MR. Radiosynthesis and in vivo evaluation of 11C-labeled BMS-193885 and its desmethyl analog as PET tracers for neuropeptide Y1 receptors. EJNMMI Radiopharm Chem. 2019 Feb 18;4(1):4. doi: 10.1186/s41181-019-0056-5. PMID: 31659508; PMCID: PMC6379498. 3: Wang C, Han X, Guo F, Sun X, Luan X, Xu L. Orexin-A signaling in the paraventricular nucleus modulates spontaneous firing of glucose-sensitive neurons and promotes food intake via the NPY pathway in rats. Biochem Biophys Res Commun. 2018 Oct 20;505(1):162-167. doi: 10.1016/j.bbrc.2018.09.091. Epub 2018 Sep 20. PMID: 30243725. 4: Yang Z, Han S, Keller M, Kaiser A, Bender BJ, Bosse M, Burkert K, Kögler LM, Wifling D, Bernhardt G, Plank N, Littmann T, Schmidt P, Yi C, Li B, Ye S, Zhang R, Xu B, Larhammar D, Stevens RC, Huster D, Meiler J, Zhao Q, Beck-Sickinger AG, Buschauer A, Wu B. Structural basis of ligand binding modes at the neuropeptide Y Y1 receptor. Nature. 2018 Apr;556(7702):520-524. doi: 10.1038/s41586-018-0046-x. Epub 2018 Apr 18. PMID: 29670288; PMCID: PMC5920736. 5: Hussain S, Richardson E, Ma Y, Holton C, De Backer I, Buckley N, Dhillo W, Bewick G, Zhang S, Carling D, Bloom S, Gardiner J. Glucokinase activity in the arcuate nucleus regulates glucose intake. J Clin Invest. 2015 Jan;125(1):337-49. doi: 10.1172/JCI77172. Epub 2014 Dec 8. PMID: 25485685; PMCID: PMC4382228. 6: Kaczyńska K, Szereda-Przestaszewska M. Activation of neuropeptide Y(2) receptors exerts an excitatory action on cardio-respiratory variables in anaesthetized rats. Neuropeptides. 2011 Aug;45(4):281-6. doi: 10.1016/j.npep.2011.05.003. Epub 2011 Jun 11. PMID: 21658765. 7: Kaczyńska K, Szereda-Przestaszewska M. NPY Y(1) receptors are involved in cardio-respiratory responses to intravenous injection of neuropeptide Y in anaesthetized rats. Pharmacol Res. 2010 Nov;62(5):444-9. doi: 10.1016/j.phrs.2010.06.006. Epub 2010 Jun 17. PMID: 20600918. 8: Antal-Zimanyi I, Bruce MA, Leboulluec KL, Iben LG, Mattson GK, McGovern RT, Hogan JB, Leahy CL, Flowers SC, Stanley JA, Ortiz AA, Poindexter GS. Pharmacological characterization and appetite suppressive properties of BMS-193885, a novel and selective neuropeptide Y(1) receptor antagonist. Eur J Pharmacol. 2008 Aug 20;590(1-3):224-32. doi: 10.1016/j.ejphar.2008.06.032. Epub 2008 Jun 12. PMID: 18573246. 9: Poindexter GS, Bruce MA, Breitenbucher JG, Higgins MA, Sit SY, Romine JL, Martin SW, Ward SA, McGovern RT, Clarke W, Russell J, Antal-Zimanyi I. Dihydropyridine neuropeptide Y Y1 receptor antagonists 2. bioisosteric urea replacements. Bioorg Med Chem. 2004 Jan 15;12(2):507-21. doi: 10.1016/j.bmc.2003.10.016. PMID: 14723969. 10: Poindexter GS, Bruce MA, LeBoulluec KL, Monkovic I, Martin SW, Parker EM, Iben LG, McGovern RT, Ortiz AA, Stanley JA, Mattson GK, Kozlowski M, Arcuri M, Antal-Zimanyi I. Dihydropyridine neuropeptide Y Y(1) receptor antagonists. Bioorg Med Chem Lett. 2002 Feb 11;12(3):379-82. doi: 10.1016/s0960-894x(01)00761-2. PMID: 11814801.