SR-17018 | CAS#2134602-45-0 | MOR agonist

MedKoo Cat#: 555270 | Name: SR-17018

Description:

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

SR-17018 is a biased mu-opioid receptor (MOR) agonist that exhibits unique pharmacological properties compared to conventional opioids. It demonstrates high binding affinity for MOR (K𝑖 ~ 18 nM) with preferential G-protein signaling over β-arrestin recruitment, which is proposed to reduce adverse effects such as respiratory depression and tolerance. Functional assays show that SR-17018 has an EC50 of approximately 80 nM for G-protein activation, with a significantly reduced efficacy for β-arrestin recruitment compared to morphine. In vivo, SR-17018 produces dose-dependent analgesia in rodent pain models while displaying a slow onset and prolonged duration of action.

Chemical Structure

SR-17018

CAS#2134602-45-0

Theoretical Analysis

MedKoo Cat#: 555270

Name: SR-17018

CAS#: 2134602-45-0

Chemical Formula: C19H18Cl3N3O

Exact Mass: 409.0515

Molecular Weight: 410.72

Elemental Analysis: C, 55.56; H, 4.42; Cl, 25.89; N, 10.23; O, 3.90

Price and Availability

Size	Price	Availability
10mg	USD 150.00	Ready to ship
25mg	USD 250.00	Ready to ship
50mg	USD 450.00	Ready to ship
100mg	USD 750.00	Ready to ship

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Related CAS #

No Data

Synonym

SR17018; SR-17018; SR 17018;

IUPAC/Chemical Name

5,6-dichloro-1-(1-(4-chlorobenzyl)piperidin-4-yl)-1,3-dihydro-2H-benzo[d]imidazol-2-one

InChi Key

LAGUDYUGRSQDKS-UHFFFAOYSA-N

InChi Code

InChI=1S/C19H18Cl3N3O/c20-13-3-1-12(2-4-13)11-24-7-5-14(6-8-24)25-18-10-16(22)15(21)9-17(18)23-19(25)26/h1-4,9-10,14H,5-8,11H2,(H,23,26)

SMILES Code

C1=CC(CN2CCC(N3C(=O)NC4C=C(Cl)C(Cl)=CC3=4)CC2)=CC=C1Cl

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

Certificate of Analysis

View CoA: current batch, Lot#A8T08K13

QC Data

View QC data: current batch, Lot#A8T08K13

Safety Data Sheet (SDS)

View Safety Data Sheet (SDS)

Instruction

View handling instruction

Biological target:

SR-17018 is an mu-opioid-receptor (MOR) agonist, binding with GTPγS, with an EC50 of 97 nM.

In vitro activity:

To be determined

In vivo activity:

Biased agonists, such as SR-17018, may be useful for opioid dependence treatment, while also restoring opioid antinociceptive sensitivity. When chronically administered to mice, SR-17018 did not lead to certain hallmarks of opioid neuronal adaptations seen with morphine. Substitution with SR-17018 in morphine-tolerant mice restored morphine potency and efficacy, whereas the onset of opioid withdrawal was prevented. Reference: Neuropsychopharmacology. 2020 Jan; 45(2): 416–425. https://pubmed.ncbi.nlm.nih.gov/31443104/

	Solvent	mg/mL	mM	comments
Solubility
	DMSO	6.0	14.61

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 410.72 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. Hill R, Sanchez J, Lemel L, Antonijevic M, Hosking Y, Mistry SN, Kruegel AC, Javitch JA, Lane JR, Canals M. Assessment of the potential of novel and classical opioids to induce respiratory depression in mice. Br J Pharmacol. 2023 Dec;180(24):3160-3174. doi: 10.1111/bph.16199. Epub 2023 Aug 22. PMID: 37489013. 2. Grim TW, Schmid CL, Stahl EL, Pantouli F, Ho JH, Acevedo-Canabal A, Kennedy NM, Cameron MD, Bannister TD, Bohn LM. A G protein signaling-biased agonist at the μ-opioid receptor reverses morphine tolerance while preventing morphine withdrawal. Neuropsychopharmacology. 2020 Jan;45(2):416-425. doi: 10.1038/s41386-019-0491-8. Epub 2019 Aug 23. PMID: 31443104; PMCID: PMC6901606.

In vitro protocol:

To be determined

In vivo protocol:

1: Grim TW, Schmid CL, Stahl EL, Pantouli F, Ho JH, Acevedo-Canabal A, Kennedy NM, Cameron MD, Bannister TD, Bohn LM. A G protein signaling-biased agonist at the μ-opioid receptor reverses morphine tolerance while preventing morphine withdrawal. Neuropsychopharmacology. 2020 Jan;45(2):416-425. doi: 10.1038/s41386-019-0491-8. Epub 2019 Aug 23. PMID: 31443104; PMCID: PMC6901606. 2: Gillis A, Gondin AB, Kliewer A, Sanchez J, Lim HD, Alamein C, Manandhar P, Santiago M, Fritzwanker S, Schmiedel F, Katte TA, Reekie T, Grimsey NL, Kassiou M, Kellam B, Krasel C, Halls ML, Connor M, Lane JR, Schulz S, Christie MJ, Canals M. Low intrinsic efficacy for G protein activation can explain the improved side effect profiles of new opioid agonists. Sci Signal. 2020 Mar 31;13(625):eaaz3140. doi: 10.1126/scisignal.aaz3140. PMID: 32234959. 3: Azevedo Neto J, Costanzini A, De Giorgio R, Lambert DG, Ruzza C, Calò G. Biased versus Partial Agonism in the Search for Safer Opioid Analgesics. Molecules. 2020 Aug 25;25(17):3870. doi: 10.3390/molecules25173870. PMID: 32854452; PMCID: PMC7504468. 4: Podlewska S, Bugno R, Kudla L, Bojarski AJ, Przewlocki R. Molecular Modeling of µ Opioid Receptor Ligands with Various Functional Properties: PZM21, SR-17018, Morphine, and Fentanyl-Simulated Interaction Patterns Confronted with Experimental Data. Molecules. 2020 Oct 12;25(20):4636. doi: 10.3390/molecules25204636. PMID: 33053718; PMCID: PMC7594085. 5: Pantouli F, Grim TW, Schmid CL, Acevedo-Canabal A, Kennedy NM, Cameron MD, Bannister TD, Bohn LM. Comparison of morphine, oxycodone and the biased MOR agonist SR-17018 for tolerance and efficacy in mouse models of pain. Neuropharmacology. 2021 Mar 1;185:108439. doi: 10.1016/j.neuropharm.2020.108439. Epub 2020 Dec 17. PMID: 33345829; PMCID: PMC7887086. 6: Fritzwanker S, Schulz S, Kliewer A. SR-17018 Stimulates Atypical µ-Opioid Receptor Phosphorylation and Dephosphorylation. Molecules. 2021 Jul 27;26(15):4509. doi: 10.3390/molecules26154509. PMID: 34361663; PMCID: PMC8348759. 7: Stahl EL, Bohn LM. Low Intrinsic Efficacy Alone Cannot Explain the Improved Side Effect Profiles of New Opioid Agonists. Biochemistry. 2022 Sep 20;61(18):1923-1935. doi: 10.1021/acs.biochem.1c00466. Epub 2021 Sep 1. PMID: 34468132; PMCID: PMC8885792. 8: Stahl EL, Schmid CL, Acevedo-Canabal A, Read C, Grim TW, Kennedy NM, Bannister TD, Bohn LM. G protein signaling-biased mu opioid receptor agonists that produce sustained G protein activation are noncompetitive agonists. Proc Natl Acad Sci U S A. 2021 Nov 30;118(48):e2102178118. doi: 10.1073/pnas.2102178118. PMID: 34819362; PMCID: PMC8640941. 9: Kudla L, Bugno R, Podlewska S, Szumiec L, Wiktorowska L, Bojarski AJ, Przewlocki R. Comparison of an Addictive Potential of μ-Opioid Receptor Agonists with G Protein Bias: Behavioral and Molecular Modeling Studies. Pharmaceutics. 2021 Dec 27;14(1):55. doi: 10.3390/pharmaceutics14010055. PMID: 35056950; PMCID: PMC8779292. 10: Acevedo-Canabal A, Grim TW, Schmid CL, McFague N, Stahl EL, Kennedy NM, Bannister TD, Bohn LM. Hyperactivity in Mice Induced by Opioid Agonists with Partial Intrinsic Efficacy and Biased Agonism Administered Alone and in Combination with Morphine. Biomolecules. 2023 Jun 2;13(6):935. doi: 10.3390/biom13060935. PMID: 37371516; PMCID: PMC10295947. 11: Hill R, Sanchez J, Lemel L, Antonijevic M, Hosking Y, Mistry SN, Kruegel AC, Javitch JA, Lane JR, Canals M. Assessment of the potential of novel and classical opioids to induce respiratory depression in mice. Br J Pharmacol. 2023 Dec;180(24):3160-3174. doi: 10.1111/bph.16199. Epub 2023 Aug 22. PMID: 37489013; PMCID: PMC10952895. 12: Singleton S, Dieterle C, Walker DJ, Runeberg T, Oswald AS, Rosenqvist G, Robertson L, McCarthy T, Sarkar S, Baptista-Hon D, Hales TG. Activation of μ receptors by SR-17018 through a distinctive mechanism. Neuropharmacology. 2024 Nov 1;258:110093. doi: 10.1016/j.neuropharm.2024.110093. Epub 2024 Jul 25. PMID: 39067665.