RXFP3/4-Agonist-1

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

MedKoo CAT#: 565725

CAS#: N/A

Description: RXFP3/4-Agonist-1 is a the first small molecule rxfp3/4 agonist, increasing food intake in rats upon acute central administration


Chemical Structure

img
RXFP3/4-Agonist-1
CAS# N/A

Theoretical Analysis

MedKoo Cat#: 565725
Name: RXFP3/4-Agonist-1
CAS#: N/A
Chemical Formula: C20H22ClN5O
Exact Mass: 0.00
Molecular Weight: 0.000
Elemental Analysis: Elemental Analysis: C, 62.58; H, 5.78; Cl, 9.23; N, 18.24; O, 4.17

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

Request quote for custom synthesis

Synonym: RXFP3/4-Agonist-1

IUPAC/Chemical Name: (E)-N-(4-Chlorophenethyl)-2-((7-ethyl-5-hydroxy-1H-indol-3-yl)methylene)hydrazine-1-carboximidamide

InChi Key: NQWXHRRWWPCDAJ-BRJLIKDPSA-N

InChi Code: InChI=1S/C20H22ClN5O/c1-2-14-9-17(27)10-18-15(11-24-19(14)18)12-25-26-20(22)23-8-7-13-3-5-16(21)6-4-13/h3-6,9-12,24,27H,2,7-8H2,1H3,(H3,22,23,26)/b25-12+

SMILES Code: N=C(N/N=C/C1=CNC2=C1C=C(O)C=C2CC)NCCC3=CC=C(Cl)C=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: >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:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 0.00 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:
In vitro protocol:
In vivo protocol:

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

1: Kristensson L, Mayer G, Ploj K, Wetterlund M, Arlbrandt S, Björquist A, Wissing BM, Castaldo M, Larsson N. Partial agonist activity of R3(BΔ23-27)R/I5 at RXFP3--investigation of in vivo and in vitro pharmacology. Eur J Pharmacol. 2015 Jan 15;747:123-31. doi: 10.1016/j.ejphar.2014.11.041. Epub 2014 Dec 11. PubMed PMID: 25496752.

2: Wong LLL, Scott DJ, Hossain MA, Kaas Q, Rosengren KJ, Bathgate RAD. Distinct but overlapping binding sites of agonist and antagonist at the relaxin family peptide 3 (RXFP3) receptor. J Biol Chem. 2018 Oct 12;293(41):15777-15789. doi: 10.1074/jbc.RA118.002645. Epub 2018 Aug 21. PubMed PMID: 30131340; PubMed Central PMCID: PMC6187618.

3: Wei D, Hu MJ, Shao XX, Wang JH, Nie WH, Liu YL, Xu ZG, Guo ZY. Development of a selective agonist for relaxin family peptide receptor 3. Sci Rep. 2017 Jun 12;7(1):3230. doi: 10.1038/s41598-017-03465-7. PubMed PMID: 28607363; PubMed Central PMCID: PMC5468247.

4: DeChristopher B, Park SH, Vong L, Bamford D, Cho HH, Duvadie R, Fedolak A, Hogan C, Honda T, Pandey P, Rozhitskaya O, Su L, Tomlinson E, Wallace I. Discovery of a small molecule RXFP3/4 agonist that increases food intake in rats upon acute central administration. Bioorg Med Chem Lett. 2019 Apr 15;29(8):991-994. doi: 10.1016/j.bmcl.2019.02.013. Epub 2019 Feb 11. PubMed PMID: 30824200.

5: Heidari S, Taromchi AH, Nejatbakhsh R, Shokri S. Expression and localisation of RXFP3 in human spermatozoa and impact of INSL7 on sperm functions. Andrologia. 2018 Apr;50(3). doi: 10.1111/and.12928. Epub 2017 Nov 21. PubMed PMID: 29159832.

6: Ma S, Smith CM, Blasiak A, Gundlach AL. Distribution, physiology and pharmacology of relaxin-3/RXFP3 systems in brain. Br J Pharmacol. 2017 May;174(10):1034-1048. doi: 10.1111/bph.13659. Epub 2016 Dec 4. Review. PubMed PMID: 27774604; PubMed Central PMCID: PMC5406293.

7: Albert-Gascó H, García-Avilés Á, Moustafa S, Sánchez-Sarasua S, Gundlach AL, Olucha-Bordonau FE, Sánchez-Pérez AM. Central relaxin-3 receptor (RXFP3) activation increases ERK phosphorylation in septal cholinergic neurons and impairs spatial working memory. Brain Struct Funct. 2017 Jan;222(1):449-463. doi: 10.1007/s00429-016-1227-8. Epub 2016 May 5. PubMed PMID: 27146679.

8: Kania A, Gugula A, Grabowiecka A, de Ávila C, Blasiak T, Rajfur Z, Lewandowski MH, Hess G, Timofeeva E, Gundlach AL, Blasiak A. Inhibition of oxytocin and vasopressin neuron activity in rat hypothalamic paraventricular nucleus by relaxin-3-RXFP3 signalling. J Physiol. 2017 Jun 1;595(11):3425-3447. doi: 10.1113/JP273787. Epub 2017 Feb 27. PubMed PMID: 28098344; PubMed Central PMCID: PMC5451722.

9: Smith CM, Blasiak A, Ganella DE, Chua BE, Layfield SL, Bathgate RA, Gundlach AL. Viral-mediated delivery of an RXFP3 agonist into brain promotes arousal in mice. Ital J Anat Embryol. 2013;118(1 Suppl):42-6. PubMed PMID: 24640570.

10: Zhang X, Pan L, Yang K, Fu Y, Liu Y, Chen W, Ma X, Yin X. Alterations of relaxin and its receptor system components in experimental diabetic cardiomyopathy rats. Cell Tissue Res. 2017 Nov;370(2):297-304. doi: 10.1007/s00441-017-2662-4. Epub 2017 Aug 3. PubMed PMID: 28776188.

11: Haidar M, Guèvremont G, Zhang C, Bathgate RAD, Timofeeva E, Smith CM, Gundlach AL. Relaxin-3 inputs target hippocampal interneurons and deletion of hilar relaxin-3 receptors in "floxed-RXFP3" mice impairs spatial memory. Hippocampus. 2017 May;27(5):529-546. doi: 10.1002/hipo.22709. Epub 2017 Jan 31. PubMed PMID: 28100033.

12: de Ávila C, Chometton S, Lenglos C, Calvez J, Gundlach AL, Timofeeva E. Differential effects of relaxin-3 and a selective relaxin-3 receptor agonist on food and water intake and hypothalamic neuronal activity in rats. Behav Brain Res. 2018 Jan 15;336:135-144. doi: 10.1016/j.bbr.2017.08.044. Epub 2017 Aug 31. PubMed PMID: 28864207.

13: Zhang C, Baimoukhametova DV, Smith CM, Bains JS, Gundlach AL. Relaxin-3/RXFP3 signalling in mouse hypothalamus: no effect of RXFP3 activation on corticosterone, despite reduced presynaptic excitatory input onto paraventricular CRH neurons in vitro. Psychopharmacology (Berl). 2017 Jun;234(11):1725-1739. doi: 10.1007/s00213-017-4575-z. Epub 2017 Mar 17. PubMed PMID: 28314951.

14: Albert-Gascó H, Ma S, Ros-Bernal F, Sánchez-Pérez AM, Gundlach AL, Olucha-Bordonau FE. GABAergic Neurons in the Rat Medial Septal Complex Express Relaxin-3 Receptor (RXFP3) mRNA. Front Neuroanat. 2018 Jan 17;11:133. doi: 10.3389/fnana.2017.00133. eCollection 2017. PubMed PMID: 29403361; PubMed Central PMCID: PMC5777284.

15: Halls ML, Bathgate RA, Sutton SW, Dschietzig TB, Summers RJ. International Union of Basic and Clinical Pharmacology. XCV. Recent advances in the understanding of the pharmacology and biological roles of relaxin family peptide receptors 1-4, the receptors for relaxin family peptides. Pharmacol Rev. 2015;67(2):389-440. doi: 10.1124/pr.114.009472. Review. PubMed PMID: 25761609; PubMed Central PMCID: PMC4394689.

16: Zhang C, Chua BE, Yang A, Shabanpoor F, Hossain MA, Wade JD, Rosengren KJ, Smith CM, Gundlach AL. Central relaxin-3 receptor (RXFP3) activation reduces elevated, but not basal, anxiety-like behaviour in C57BL/6J mice. Behav Brain Res. 2015 Oct 1;292:125-32. doi: 10.1016/j.bbr.2015.06.010. Epub 2015 Jun 6. PubMed PMID: 26057358.

17: Lee JH, Koh SQ, Guadagna S, Francis PT, Esiri MM, Chen CP, Wong PT, Dawe GS, Lai MK. Altered relaxin family receptors RXFP1 and RXFP3 in the neocortex of depressed Alzheimer's disease patients. Psychopharmacology (Berl). 2016 Feb;233(4):591-8. doi: 10.1007/s00213-015-4131-7. Epub 2015 Nov 6. PubMed PMID: 26542729.

18: Ryan PJ, Kastman HE, Krstew EV, Rosengren KJ, Hossain MA, Churilov L, Wade JD, Gundlach AL, Lawrence AJ. Relaxin-3/RXFP3 system regulates alcohol-seeking. Proc Natl Acad Sci U S A. 2013 Dec 17;110(51):20789-94. doi: 10.1073/pnas.1317807110. Epub 2013 Dec 2. PubMed PMID: 24297931; PubMed Central PMCID: PMC3870696.

19: Haidar M, Lam M, Chua BE, Smith CM, Gundlach AL. Sensitivity to Chronic Methamphetamine Administration and Withdrawal in Mice with Relaxin-3/RXFP3 Deficiency. Neurochem Res. 2016 Mar;41(3):481-91. doi: 10.1007/s11064-015-1621-2. Epub 2015 May 29. PubMed PMID: 26023064.

20: Smith CM, Walker LL, Chua BE, McKinley MJ, Gundlach AL, Denton DA, Lawrence AJ. Involvement of central relaxin-3 signalling in sodium (salt) appetite. Exp Physiol. 2015 Sep;100(9):1064-72. doi: 10.1113/EP085349. Epub 2015 Jul 27. PubMed PMID: 26147879.