MedKoo Biosciences, Inc.
Tel:   +1-919-636-5577    Fax:   +1-919-980-4831    Email:   sales@medkoo.com
Search
Login Register
Search
MedKoo Cat#: 531471 | Name: AR-M1000390 HCl
Featured New

Description:

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

AR-M1000390, also known as ARM-390, is a nonpeptidic δ receptor selective agonist.

Chemical Structure

AR-M1000390 HCl
AR-M1000390 HCl
CAS#209808-47-9 (HCl)

Theoretical Analysis

MedKoo Cat#: 531471

Name: AR-M1000390 HCl

CAS#: 209808-47-9 (HCl)

Chemical Formula: C23H29ClN2O

Exact Mass: 0.0000

Molecular Weight: 384.95

Elemental Analysis: C, 71.76; H, 7.59; Cl, 9.21; N, 7.28; O, 4.16

Price and Availability

Size Price Availability Quantity
10mg USD 150.00 Ready to ship
25mg USD 250.00 Ready to ship
50mg USD 425.00 Ready to ship
100mg USD 750.00 Ready to ship
200mg USD 1,250.00 Ready to ship
500mg USD 2,450.00 Ready to ship
1g USD 3,450.00 2 Weeks
Show More
Bulk Inquiry
Buy Now
Add to Cart
Related CAS #
209808-47-9 (HCl) 209808-01-5 (free base)
Synonym
AR-M1000390; ARM1000390; AR M1000390; ARM-390; ARM 390; ARM390; ARM-390 hydrochloride.
IUPAC/Chemical Name
N,N-diethyl-4-(phenyl-piperidin-4-ylidenemethyl)benzamide hydrochloride.
InChi Key
OTXTZCLQEGSAMW-UHFFFAOYSA-N
InChi Code
InChI=1S/C23H28N2O.ClH/c1-3-25(4-2)23(26)21-12-10-19(11-13-21)22(18-8-6-5-7-9-18)20-14-16-24-17-15-20;/h5-13,24H,3-4,14-17H2,1-2H3;1H
SMILES Code
O=C(N(CC)CC)C1=CC=C(/C(C2=CC=CC=C2)=C3CCNCC/3)C=C1.[H]Cl
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
More Info
Biological target:
AR-M 1000390 hydrochloride is a δ opioid receptor agonist with an EC50 of 7.2±0.9 nM for δ agonist potency.
In vitro activity:
N/A
In vivo activity:
In a separate group of animals, a maximal doses of ARM390 (10 mg·kg−1) also reversed NTG-induce mechanical hyperalgesia, comparable to the effect of SNC80 (10 mg·kg−1, Figure 1B). In addition, systemic administration of NTG also induced heat hyperalgesia (Figure 1C, VEH vs. dashed line), which was also reversed by both SNC80 and ARM390 (Figure 1C). This study further examined the selectivity of both δ-agonists in the NTG model, by testing δ-opioid receptor wild-type and knockout mice. This study found that the effects of SNC80 and ARM390 in reversing NTG-induced mechanical hyperalgesia in wild-type mice were absent in the δ-receptor knockout animals (Figure 1D). In addition, the δ-opioid receptor antagonist, naltrindole, blocked the anti-hyperalgesic effects of SNC80 and ARM390 in wild-type mice (Supporting Information Fig. S1). Thus, selective δ-opioid receptor agonists reverse sensory hypersensitivity in the NTG model of migraine pain. Reference: Br J Pharmacol. 2014 May; 171(9): 2375–2384. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3997277/
Solvent mg/mL mM
Solubility
DMSO 94.3 244.84
Water 38.5 99.99
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 384.95 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:
N/A
In vitro protocol:
N/A
In vivo protocol:
1. Pradhan AA, Smith ML, Zyuzin J, Charles A. δ-Opioid receptor agonists inhibit migraine-related hyperalgesia, aversive state and cortical spreading depression in mice. Br J Pharmacol. 2014 May;171(9):2375-84. doi: 10.1111/bph.12591. PMID: 24467301; PMCID: PMC3997277.
1: Nozaki C, Nagase H, Nemoto T, Matifas A, Kieffer BL, Gaveriaux-Ruff C. In vivo properties of KNT-127, a novel δ opioid receptor agonist: receptor internalization, antihyperalgesia and antidepressant effects in mice. Br J Pharmacol. 2014 Dec;171(23):5376-86. doi: 10.1111/bph.12852. PubMed PMID: 25048778; PubMed Central PMCID: PMC4294046. 2: Pradhan AA, Walwyn W, Nozaki C, Filliol D, Erbs E, Matifas A, Evans C, Kieffer BL. Ligand-directed trafficking of the δ-opioid receptor in vivo: two paths toward analgesic tolerance. J Neurosci. 2010 Dec 8;30(49):16459-68. doi: 10.1523/JNEUROSCI.3748-10.2010. PubMed PMID: 21147985; PubMed Central PMCID: PMC3086517. 3: Pradhan AA, Becker JA, Scherrer G, Tryoen-Toth P, Filliol D, Matifas A, Massotte D, Gavériaux-Ruff C, Kieffer BL. In vivo delta opioid receptor internalization controls behavioral effects of agonists. PLoS One. 2009;4(5):e5425. doi: 10.1371/journal.pone.0005425. PubMed PMID: 19412545; PubMed Central PMCID: PMC2672171. 4: Otieno MA, Bavuso N, Milano J, Foster-Brown L, Bui KH, Li Y, Hudzik T, Wescott D, Louden C, Dyroff M, Pognan F. Mechanistic investigation of N,N-diethyl-4-(phenyl-piperidin-4-ylidenemethyl)-benzamide-induced insulin depletion in the rat and RINm5F cells. Toxicol Sci. 2008 Sep;105(1):221-9. doi: 10.1093/toxsci/kfn108. PubMed PMID: 18539914. 5: Marie N, Landemore G, Debout C, Jauzac P, Allouche S. Pharmacological characterization of AR-M1000390 at human delta opioid receptors. Life Sci. 2003 Aug 15;73(13):1691-704. PubMed PMID: 12875901. 6: Wei ZY, Brown W, Takasaki B, Plobeck N, Delorme D, Zhou F, Yang H, Jones P, Gawell L, Gagnon H, Schmidt R, Yue SY, Walpole C, Payza K, St-Onge S, Labarre M, Godbout C, Jakob A, Butterworth J, Kamassah A, Morin PE, Projean D, Ducharme J, Roberts E. N,N-Diethyl-4-(phenylpiperidin-4-ylidenemethyl)benzamide: a novel, exceptionally selective, potent delta opioid receptor agonist with oral bioavailability and its analogues. J Med Chem. 2000 Oct 19;43(21):3895-905. PubMed PMID: 11052794.