J-2156 | SST4 Agonist

J-2156
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 574069

CAS#: 2387505-73-7

Description: J-2156 is a high affinity human somatostatin receptor 4 (sst4) agonist that reduces inflammatory airway hyperresponsiveness in acute and chronic airway inflammation. J-2156 also exhibits anxiolytic effects.

Chemical Structure

J-2156

CAS# 2387505-73-7

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 574069
Name: J-2156
CAS#: 2387505-73-7
Chemical Formula: C26H29F3N4O6S
Exact Mass: 582.18
Molecular Weight: 582.595
Elemental Analysis: C, 53.60; H, 5.02; F, 9.78; N, 9.62; O, 16.48; S, 5.50

Price and Availability

Size	Price	Availability
5mg	USD 350	2 Weeks
10mg	USD 600	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: J-2156, J2156, J 2156

IUPAC/Chemical Name: (1'S,2S)-4-Amino-N-(1'-carbamoyl-2'-phenylethyl)-2-(4"-methyl-1"-naphthalenesulfonylamino)butanamide trifluoroacetate

InChi Key: OCEMIQKESMKGAP-GUTACTQSSA-N

InChi Code: InChI=1S/C24H28N4O4S.C2HF3O2/c1-16-11-12-22(19-10-6-5-9-18(16)19)33(31,32)28-20(13-14-25)24(30)27-21(23(26)29)15-17-7-3-2-4-8-17;3-2(4,5)1(6)7/h2-12,20-21,28H,13-15,25H2,1H3,(H2,26,29)(H,27,30);(H,6,7)/t20-,21-;/m0./s1

SMILES Code: O=C(N[C@H](C(N)=O)CC1=CC=CC=C1)[C@@H](NS(=O)(C2=C3C=CC=CC3=C(C)C=C2)=O)CCN.O=C(O)C(F)(F)F

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:	J-2156 TFA is a high potent, selective somatostatin receptor type 4 (SST4 receptor) agonist with IC50s of 0.05 nM and 0.07 nM for human and rat SST4 receptors, respectively.
In vitro activity:	J-2156 (10–2000 nm) significantly inhibited the stimulation-evoked release of all the three measured sensory neuropeptides in a concentration-dependent manner, although it did not influence basal, nonstimulated peptide release. Reference: Br J Pharmacol. 2006 Oct;149(4):405-15. https://pubmed.ncbi.nlm.nih.gov/16953190/
In vivo activity:	In LBP-rats, single intraperitoneal (i.p.) injection of J-2156 (3, 10, 30 mg kg-1) alleviated primary and secondary hyperalgesia in the lumbar axial deep tissues at L4/L5 and L1, respectively. This was accompanied by a reduction in the otherwise augmented lumbar (L4-L6) dorsal root ganglia expression levels of the pro-nociceptive mediators: phosphorylated p38 (pp38) mitogen-activated protein kinase (MAPK) and phosphorylated p44/p42 MAPK and a reduction in pp38 MAPK in the lumbar enlargement of the spinal cord. Reference: Biomed Pharmacother. 2019 Sep;117:109056. https://pubmed.ncbi.nlm.nih.gov/31181441/

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	79.1	135.82
	Water	79.1	135.82

Preparing Stock Solutions

The following data is based on the product molecular weight 582.60 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. Helyes Z, Pintér E, Németh J, Sándor K, Elekes K, Szabó A, Pozsgai G, Keszthelyi D, Kereskai L, Engström M, Wurster S, Szolcsányi J. Effects of the somatostatin receptor subtype 4 selective agonist J-2156 on sensory neuropeptide release and inflammatory reactions in rodents. Br J Pharmacol. 2006 Oct;149(4):405-15. doi: 10.1038/sj.bjp.0706876. Epub 2006 Sep 4. PMID: 16953190; PMCID: PMC1978437. 2. Park TSW, Khan N, Kuo A, Nicholson JR, Corradini L, Smith MT. J-2156, a somatostatin receptor type 4 agonist, alleviates mechanical hyperalgesia in a rat model of chronic low back pain. Biomed Pharmacother. 2019 Sep;117:109056. doi: 10.1016/j.biopha.2019.109056. Epub 2019 Jun 7. PMID: 31181441. 3. Shenoy PA, Kuo A, Khan N, Gorham L, Nicholson JR, Corradini L, Vetter I, Smith MT. The Somatostatin Receptor-4 Agonist J-2156 Alleviates Mechanical Hypersensitivity in a Rat Model of Breast Cancer Induced Bone Pain. Front Pharmacol. 2018 May 15;9:495. doi: 10.3389/fphar.2018.00495. PMID: 29867498; PMCID: PMC5962878.
In vitro protocol:	1. Helyes Z, Pintér E, Németh J, Sándor K, Elekes K, Szabó A, Pozsgai G, Keszthelyi D, Kereskai L, Engström M, Wurster S, Szolcsányi J. Effects of the somatostatin receptor subtype 4 selective agonist J-2156 on sensory neuropeptide release and inflammatory reactions in rodents. Br J Pharmacol. 2006 Oct;149(4):405-15. doi: 10.1038/sj.bjp.0706876. Epub 2006 Sep 4. PMID: 16953190; PMCID: PMC1978437.
In vivo protocol:	1. Park TSW, Khan N, Kuo A, Nicholson JR, Corradini L, Smith MT. J-2156, a somatostatin receptor type 4 agonist, alleviates mechanical hyperalgesia in a rat model of chronic low back pain. Biomed Pharmacother. 2019 Sep;117:109056. doi: 10.1016/j.biopha.2019.109056. Epub 2019 Jun 7. PMID: 31181441. 2. Shenoy PA, Kuo A, Khan N, Gorham L, Nicholson JR, Corradini L, Vetter I, Smith MT. The Somatostatin Receptor-4 Agonist J-2156 Alleviates Mechanical Hypersensitivity in a Rat Model of Breast Cancer Induced Bone Pain. Front Pharmacol. 2018 May 15;9:495. doi: 10.3389/fphar.2018.00495. PMID: 29867498; PMCID: PMC5962878.

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Engström et al (2005) Superagonism at the human somatostatin receptor subtype 4. J.Pharmacol.Exp.Ther. 312 332 PMID: 15333679

Elekes et al (2008) Inhibitory effects of synthetic somatostatin receptor subtype 4 agonists on acute and chronic airway inflammation and hyperreactivity in the mouse. Eur.J.Pharmacol. 578 313 PMID: 17961545

Scheich et al (2016) Somatostatin receptor subtype 4 activation is involved in anxiety and depression-like behavior in mouse models. Neuropharmacology. 101 204 PMID: 26387439

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