LY2087101 | CAS#913186-74-0

MedKoo Cat#: 532150 | Name: LY2087101

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Description:

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

LY2087101 is an allosteric potentiator of α7, α4β2 and α4β4 nAChRs. LY2087101 displays selectivity against α3β4 nAChRs.

Chemical Structure

LY2087101

CAS#913186-74-0

Theoretical Analysis

MedKoo Cat#: 532150

Name: LY2087101

CAS#: 913186-74-0

Chemical Formula: C15H11FN2OS2

Exact Mass: 318.0297

Molecular Weight: 318.38

Elemental Analysis: C, 56.59; H, 3.48; F, 5.97; N, 8.80; O, 5.03; S, 20.14

Price and Availability

Size	Price	Availability	Quantity
5mg	USD 350.00	2 weeks
25mg	USD 850.00	2 weeks

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Synonym

LY2087101; LY 2087101; LY-2087101.

IUPAC/Chemical Name

N-(4-fluorophenyl)-4-methyl-5-[(thiophen-3-yl)carbonyl]-1,3-thiazol-2-amine

InChi Key

PEAMDZVDNYENPN-UHFFFAOYSA-N

InChi Code

InChI=1S/C15H11FN2OS2/c1-9-14(13(19)10-6-7-20-8-10)21-15(17-9)18-12-4-2-11(16)3-5-12/h2-8H,1H3,(H,17,18)

SMILES Code

O=C(C1=C(C)N=C(NC2=CC=C(F)C=C2)S1)C3=CSC=C3

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

>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

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Product Data

Product Data

Instruction

View handling instruction

Biological target:

LY 2087101 is an allosteric potentiator of α7, α4β2 and α4β4 nAChRs; displays selectivity against α3β4 nAChRs.

In vitro activity:

LY2087101 potentiated ACh-induced currents of low-sensitivity (α4)3(β2)2 and high-sensitivity (α4)2(β2)3 nAChRs with similar potencies albeit to a different maximum potentiation (potentiation I max = ~840 and 450%, respectively). Reference: Sci Rep. 2018 Jan 19;8(1):1249. https://pubmed.ncbi.nlm.nih.gov/29352227/

In vivo activity:

In rat TCN synaptosomes, spontaneous [(3)H]D-Asp release was increased by nicotine and the nicotinic receptor agonists (±)epibatidine and RJR2403. The increase was potentiated by the positive allosteric modulator of nAChRs LY2087101, inhibited by the nicotinic antagonists mecamylamine (MEC) and dihydro-β-erythroidine hydrobromide (DHβE), and unaffected by α-bungarotoxin (α-BgTx) and methyllycaconitine (MLA). Reference: Neurochem Int. 2015 Nov;90:166-72. https://pubmed.ncbi.nlm.nih.gov/26277383/

	Solvent	mg/mL	mM
Solubility
	Ethanol	3.2	10.00

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 318.38 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. Deba F, Ali HI, Tairu A, Ramos K, Ali J, Hamouda AK. LY2087101 and dFBr share transmembrane binding sites in the (α4)3(β2)2 Nicotinic Acetylcholine Receptor. Sci Rep. 2018 Jan 19;8(1):1249. doi: 10.1038/s41598-018-19790-4. PMID: 29352227; PMCID: PMC5775429. 2. Samengo IA, Currò D, Martire M. Nicotinic receptors modulate the function of presynaptic AMPA receptors on glutamatergic nerve terminals in the trigeminal caudal nucleus. Neurochem Int. 2015 Nov;90:166-72. doi: 10.1016/j.neuint.2015.08.008. Epub 2015 Aug 12. PMID: 26277383.

In vitro protocol:

In vivo protocol:

1. Samengo IA, Currò D, Martire M. Nicotinic receptors modulate the function of presynaptic AMPA receptors on glutamatergic nerve terminals in the trigeminal caudal nucleus. Neurochem Int. 2015 Nov;90:166-72. doi: 10.1016/j.neuint.2015.08.008. Epub 2015 Aug 12. PMID: 26277383.

1: Wang J, Lindstrom J. Orthosteric and Allosteric Potentiation of Heteromeric Neuronal Nicotinic Acetylcholine Receptors. Br J Pharmacol. 2017 Feb 15. doi: 10.1111/bph.13745. [Epub ahead of print] Review. PubMed PMID: 28199738. 2: Samengo IA, Currò D, Martire M. Nicotinic receptors modulate the function of presynaptic AMPA receptors on glutamatergic nerve terminals in the trigeminal caudal nucleus. Neurochem Int. 2015 Nov;90:166-72. doi: 10.1016/j.neuint.2015.08.008. PubMed PMID: 26277383.