WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 555270
Description: SR17018 is an mu-opioid-receptor (MOR) agonist with an EC50 of 97 nM.
MedKoo Cat#: 555270
Chemical Formula: C19H18Cl3N3O
Exact Mass: 409.0515
Molecular Weight: 410.723
Elemental Analysis: C, 55.56; H, 4.42; Cl, 25.89; N, 10.23; O, 3.90
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
|Biological target:||SR17018 is an mu-opioid-receptor (MOR) agonist, binding with GTPγS, with an EC50 of 97 nM.|
|In vitro activity:||TBD|
|In vivo activity:||The onset of tolerance and dependence for oxycodone was tested and assessed for neurochemical changes associated with prolonged treatment with the biased agonist SR-17018. Male C57BL/6 mice treated for 6 days with SR-17018 at 24 mg/kg/day produces no tolerance, whereas a slight decrease in potency is observed when administered at 48 mg/kg/day. Female mice, treated in the same manner with SR-17018 at 48 mg/kg/day, do not display tolerance (Supplementary Fig. 2 and Table 1). MOR activation was intact in SR-17018-treated mice compared with vehicle-treated mice (Fig. 1g, h). For the SR-17018-treated group, no signs of withdrawal were observed at 3 and 6 h after the last 24 mg/kg, p.o. dose of SR-17018, which is consistent with the pharmacokinetic data supporting the presence of SR-17018 at 6 h (Fig. 2b, Fig. 1a, and Supplementary Fig. 1A,B). Withdrawal signs presented at 13 h after the last p.o. dose of SR-17018 and were recorded for 3 days at the time shown (Fig. 2b). A comparison of the sum of the withdrawal signs collected from the first signs of withdrawal over 3 days (from 1 to 72 h for morphine and from 13 to 84 h for SR-17018) to their respective controls demonstrates that chronic treatment with either compound produces significant withdrawal (morphine vs. saline; p < 0.05; SR-17018 vs. vehicle, p < 0.01, two-way ANOVA, Fig. 2a, b). The SR-17018-treated animals return to vehicle control levels by 48 h, whereas the morphine-treated group continue to show signs of withdrawal 3 days after the initial onset of withdrawal as compared with saline-treated mice.This proposes that SR-17018 has the characteristics of performing as a stabilizing agonist at MOR whereupon chronic treatment stabilizes a G protein coupling state and may represent a means to restore MOR responsiveness and analgesic efficacy in the opioid-dependent state, while lessening the severity of opiate withdrawal. Reference: Neuropsychopharmacology. 2020 Jan; 45(2): 416–425. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6901606/|
|Solvent||Max Conc. mg/mL||Max Conc. mM|
The following data is based on the product molecular weight 410.723 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. 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:||TBD|
|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.|
Schmid CL, et al. Bias Factor and Therapeutic Window Correlate to Predict Safer Opioid Analgesics. Cell. 2017 Nov 16;171(5):1165-1175.e13.