Naloxone HCl Dihydrate | CAS#51481-60-8 | opiate antagonist

Naloxone HCl Dihydrate
featured

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

MedKoo CAT#: 563433

CAS#: 51481-60-8 (HCl hydrate)

Description: Naloxone HCl Dihydrate is a specific opiate antagonist. It acts by being competitive at mu, delta, and kappa opioid receptors.

Chemical Structure

Naloxone HCl Dihydrate

CAS# 51481-60-8 (HCl hydrate)

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 563433
Name: Naloxone HCl Dihydrate
CAS#: 51481-60-8 (HCl hydrate)
Chemical Formula: C19H26ClNO6
Exact Mass: 0.00
Molecular Weight: 399.868
Elemental Analysis: C, 57.07; H, 6.55; Cl, 8.87; N, 3.50; O, 24.01

Price and Availability

Size	Price	Availability
250mg	USD 450	2 Weeks
1g	USD 1250	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: Naloxone Hydrochloride Dihydrate; Naloxone HCl Dihydrate; Naloxone HCl 2H2O;

IUPAC/Chemical Name: (4R,4aS,7aS,12bS)-3-allyl-4a,9-dihydroxy-2,3,4,4a,5,6-hexahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinolin-7(7aH)-one hydrochloride dihydrate

InChi Key: TXMZWEASFRBVKY-FERDOLAUSA-N

InChi Code: InChI=1S/C19H21NO4.ClH.2H2O/c1-2-8-20-9-7-18-15-11-3-4-12(21)16(15)24-17(18)13(22)5-6-19(18,23)14(20)10-11;;;/h2-4,14,17,21,23H,1,5-10H2;1H;2*1H2/t14-,17-,18+,19-;;;/m1.../s1

SMILES Code: O=C1[C@@H]2[C@]34C5=C(O2)C(O)=CC=C5C[C@@H](N(CC=C)CC4)[C@]3(O)CC1.[H]Cl.[H]O[H].[H]O[H]

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: 2934.99.03.00

More Info:

Product Data:

Product Data

Instruction:

View handling instruction

Biological target:	Naloxone HCl Dihydrate is a specific opiate antagonist.
In vitro activity:	The results showed that morphine directly enhanced microglia chemotaxis and membrane ruffling and that these actions were accompanied by an increase in Iba1 protein expression in the microglia, especially in the ruffling membrane. Pretreatment with 1nM (+)-naloxone significantly inhibited microglia migration, activation, and reduced Iba1 expression in microglia. On the basis of these results, Iba1 is involved in microglia migration and that ultralow dose (+)-naloxone may regulate actin cytoskeleton dynamics. Reference: J Formos Med Assoc. 2015 May;114(5):446-55. https://pubmed.ncbi.nlm.nih.gov/25649471/
In vivo activity:	The addition of naloxone at 1.0 or 2.0 µM significantly inhibited the LPS-induced production of TNFα and IL-1β (P < 0.01 for all comparisons). The lowest concentration of naloxone (0.5 µM) significantly inhibited IL-1β (P < 0.05), but not TNF-α production. Western blotting showed that p38 MAPK, JNK and ERK were constitutively present in microglia (Fig. 2A). LPS treatment induced a visible increase in the amount of P-p38 MAPK, but p38 MAPK, JNK, P-JNK, ERK and P-ERK appeared unchanged. Pretreatment with naloxone dose-dependently reversed the LPS-induced increase in P-p38 MAPK (P < 0.05, Fig. 2B). Naloxone had no significant effect on the levels of P-JNK or P-ERK (Fig. 2B). Immunofluoresence microscopy showed weak P-p38 MAPK immunostaining in OX42-positive rat microglial cells in untreated cultures (Fig. 3A). LPS-activation was accompanied by an increase in P-p38 MAPK immunostaining (Fig. 3B). Pretreatment with naloxone (Fig. 3C) resulted in P-p38 MAPK staining similar to that seen in untreated control cultures. Reference: J Int Med Res. 2012;40(4):1438-48. https://pubmed.ncbi.nlm.nih.gov/22971495/

Preparing Stock Solutions

The following data is based on the product molecular weight 399.87 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. Bimonte S, Barbieri A, Cascella M, Rea D, Palma G, Del Vecchio V, Forte CA, Del Prato F, Arra C, Cuomo A. The effects of naloxone on human breast cancer progression: in vitro and in vivo studies on MDA.MB231 cells. Onco Targets Ther. 2018 Jan 3;11:185-191. doi: 10.2147/OTT.S145780. PMID: 29379300; PMCID: PMC5757202. 2. Tsai RY, Cheng YC, Wong CS. (+)-Naloxone inhibits morphine-induced chemotaxis via prevention of heat shock protein 90 cleavage in microglia. J Formos Med Assoc. 2015 May;114(5):446-55. doi: 10.1016/j.jfma.2014.12.004. Epub 2015 Jan 31. PMID: 25649471. 3. Bimonte S, Barbieri A, Cascella M, Rea D, Palma G, Luciano A, Forte CA, Cuomo A, Arra C. Naloxone Counteracts the Promoting Tumor Growth Effects Induced by Morphine in an Animal Model of Triple-negative Breast Cancer. In Vivo. 2019 May-Jun;33(3):821-825. doi: 10.21873/invivo.11545. PMID: 31028203; PMCID: PMC6559888. 4. Xu YF, Fu LL, Jiang CH, Qin YW, Ni YQ, Fan JW. Naloxone inhibition of lipopolysaccharide-induced activation of retinal microglia is partly mediated via the p38 mitogen activated protein kinase signalling pathway. J Int Med Res. 2012;40(4):1438-48. doi: 10.1177/147323001204000422. PMID: 22971495.
In vitro protocol:	1. Bimonte S, Barbieri A, Cascella M, Rea D, Palma G, Del Vecchio V, Forte CA, Del Prato F, Arra C, Cuomo A. The effects of naloxone on human breast cancer progression: in vitro and in vivo studies on MDA.MB231 cells. Onco Targets Ther. 2018 Jan 3;11:185-191. doi: 10.2147/OTT.S145780. PMID: 29379300; PMCID: PMC5757202. 2. Tsai RY, Cheng YC, Wong CS. (+)-Naloxone inhibits morphine-induced chemotaxis via prevention of heat shock protein 90 cleavage in microglia. J Formos Med Assoc. 2015 May;114(5):446-55. doi: 10.1016/j.jfma.2014.12.004. Epub 2015 Jan 31. PMID: 25649471.
In vivo protocol:	1. Bimonte S, Barbieri A, Cascella M, Rea D, Palma G, Luciano A, Forte CA, Cuomo A, Arra C. Naloxone Counteracts the Promoting Tumor Growth Effects Induced by Morphine in an Animal Model of Triple-negative Breast Cancer. In Vivo. 2019 May-Jun;33(3):821-825. doi: 10.21873/invivo.11545. PMID: 31028203; PMCID: PMC6559888. 2. Xu YF, Fu LL, Jiang CH, Qin YW, Ni YQ, Fan JW. Naloxone inhibition of lipopolysaccharide-induced activation of retinal microglia is partly mediated via the p38 mitogen activated protein kinase signalling pathway. J Int Med Res. 2012;40(4):1438-48. doi: 10.1177/147323001204000422. PMID: 22971495.

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.

Mass

Concentration

Volume

M. Wt* 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.

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

Dilution Calculator

Calculate the dilution required to prepare a stock solution.

Concentration 1

Volume 1

Concentration 2

Volume 2

1: Chen X, Wang L, Fan S, Song S, Min H, Wu Y, He X, Liang Q, Wang Y, Yi L, Gao Q. Puerarin acts on the skeletal muscle to improve insulin sensitivity in diabetic rats involving μ-opioid receptor. Eur J Pharmacol. 2018 Jan 5;818:115-123. doi: 10.1016/j.ejphar.2017.10.033. Epub 2017 Oct 20. PubMed PMID: 29061371.

2: Dai W, Xiao D, Gao X, Zhou XB, Fang TY, Yong Z, Su RB. A brain-targeted ampakine compound protects against opioid-induced respiratory depression. Eur J Pharmacol. 2017 Aug 15;809:122-129. doi: 10.1016/j.ejphar.2017.05.025. Epub 2017 May 11. PubMed PMID: 28502631.

3: Janas A, Folwarczna J. Opioid receptor agonists may favorably affect bone mechanical properties in rats with estrogen deficiency-induced osteoporosis. Naunyn Schmiedebergs Arch Pharmacol. 2017 Feb;390(2):175-185. doi: 10.1007/s00210-016-1295-6. Epub 2016 Nov 28. PubMed PMID: 27896372; PubMed Central PMCID: PMC5233738.

4: Flint M, Than JT. Potential spawn induction and suppression agents in Caribbean Acropora cervicornis corals of the Florida Keys. PeerJ. 2016 Apr 26;4:e1982. doi: 10.7717/peerj.1982. eCollection 2016. PubMed PMID: 27168990; PubMed Central PMCID: PMC4860313.

5: Ruetzler K, Blome CJ, Nabecker S, Makarova N, Fischer H, Rinoesl H, Goliasch G, Sessler DI, Koinig H. A randomised trial of oral versus intravenous opioids for treatment of pain after cardiac surgery. J Anesth. 2014 Aug;28(4):580-6. doi: 10.1007/s00540-013-1770-x. Epub 2013 Dec 28. PubMed PMID: 24375220.

6: Sigmon SC, Dunn KE, Saulsgiver K, Patrick ME, Badger GJ, Heil SH, Brooklyn JR, Higgins ST. A randomized, double-blind evaluation of buprenorphine taper duration in primary prescription opioid abusers. JAMA Psychiatry. 2013 Dec;70(12):1347-54. doi: 10.1001/jamapsychiatry.2013.2216. PubMed PMID: 24153411; PubMed Central PMCID: PMC4131728.

7: Alford DP, LaBelle CT, Kretsch N, Bergeron A, Winter M, Botticelli M, Samet JH. Collaborative care of opioid-addicted patients in primary care using buprenorphine: five-year experience. Arch Intern Med. 2011 Mar 14;171(5):425-31. doi: 10.1001/archinternmed.2010.541. PubMed PMID: 21403039; PubMed Central PMCID: PMC3059544.

8: Mostafavi A, Abedi G, Jamshidi A, Afzali D, Talebi M. Development and validation of a HPLC method for the determination of buprenorphine hydrochloride, naloxone hydrochloride and noroxymorphone in a tablet formulation. Talanta. 2009 Feb 15;77(4):1415-9. doi: 10.1016/j.talanta.2008.09.024. Epub 2008 Sep 24. PubMed PMID: 19084658.

9: Rizzo A, Minoia G, Ceci E, Manca R, Mutinati M, Spedicato M, Sciorsci RL. The effect of calcium-naloxone treatment on blood calcium, beta-endorphin, and acetylcholine in milk fever. J Dairy Sci. 2008 Sep;91(9):3454-8. doi: 10.3168/jds.2007-0838. PubMed PMID: 18765603.

10: Berrocoso E, De Benito MD, Mico JA. Role of serotonin 5-HT1A and opioid receptors in the antiallodynic effect of tramadol in the chronic constriction injury model of neuropathic pain in rats. Psychopharmacology (Berl). 2007 Jul;193(1):97-105. Epub 2007 Mar 29. PubMed PMID: 17393145.

11: Santos AR, Miguel OG, Yunes RA, Calixto JB. Antinociceptive properties of the new alkaloid, cis-8, 10-di-N-propyllobelidiol hydrochloride dihydrate isolated from Siphocampylus verticillatus: evidence for the mechanism of action. J Pharmacol Exp Ther. 1999 Apr;289(1):417-26. PubMed PMID: 10087033.

12: Yamamoto M, Shimizu M, Okamiya H. Pharmacological actions of a new TRH analogue, YM-14673, in rats subjected to cerebral ischemia and anoxia. Eur J Pharmacol. 1990 Jun 8;181(3):207-14. PubMed PMID: 2116971.

13: Yamamoto M, Shimizu M, Ozawa Y. Effects of YM-14673, a new TRH analogue, on responses to morphine in rodents. Arch Int Pharmacodyn Ther. 1989 Jul-Aug;300:29-36. PubMed PMID: 2515820.

14: Yaksh TL, Harty GJ. Pharmacology of the allodynia in rats evoked by high dose intrathecal morphine. J Pharmacol Exp Ther. 1988 Feb;244(2):501-7. PubMed PMID: 3346833.

15: Kuriyama K, Tomono S. Significance of the enhancement of GABA receptor binding with low affinity in the assessment of central effects of benzodiazepine derivatives: Analysis using a 1H-1,2,4-triazolyl benzophenone derivative (450191-S). Neurochem Int. 1986;9(1):91-8. PubMed PMID: 20493105.

16: Woods JH, Young AM, Medzihradsky F, Smith CB, Aceto MD, Harris LS, Jacobson AE. Zomepirac: preclinical narcotic abuse liability evaluation. Arzneimittelforschung. 1983;33(2):218-22. PubMed PMID: 6133523.

Your view history

Naloxone HCl Dihydrate featured