WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H581139
CAS#: 174661-97-3
Description: DA 5018 is a capsaicin derivative, it has the antipruritic effect. DA 5018 is also a new non-narcotic analgesic.
Hodoodo Cat#: H581139
Name: DA 5018
CAS#: 174661-97-3
Chemical Formula: C22H31ClN2O3
Exact Mass: 406.20
Molecular Weight: 406.950
Elemental Analysis: C, 64.93; H, 7.68; Cl, 8.71; N, 6.88; O, 11.79
This product is not in stock, which may be available by custom synthesis.
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Synonym: DA 5018; DA-5018; DA5018;UNII-51V6N8BA2P;
IUPAC/Chemical Name: 2-(4-(2-aminoethoxy)-3-methoxyphenyl)-N-(3-(3,4-dimethylphenyl)propyl)acetamide hydrochloride
InChi Key: OUEKLNJUMVZULZ-UHFFFAOYSA-N
InChi Code: InChI=1S/C22H30N2O3.ClH/c1-16-6-7-18(13-17(16)2)5-4-11-24-22(25)15-19-8-9-20(27-12-10-23)21(14-19)26-3;/h6-9,13-14H,4-5,10-12,15,23H2,1-3H3,(H,24,25);1H
SMILES Code: NCCOc1ccc(CC(NCCCc2ccc(C)c(C)c2)=O)cc1OC.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: | |
| In vitro activity: | |
| In vivo activity: |
The following data is based on the product molecular weight 406.95 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.
| 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: |
1: Kim DH, Ahn BO, Kim SH, Kim WB. Antipruritic effect of DA-5018, a capsaicin derivative, in mice. Arch Pharm Res. 1999 Dec;22(6):549-53. PubMed PMID: 10615858.
2: Kang YS, Kim JM. Permeability of a capsaicin derivative, [14C]DA-5018 to blood-brain barrier corrected with HPLC method. Arch Pharm Res. 1999 Apr;22(2):165-72. PubMed PMID: 10230507.
3: Lee JJ, Shim HJ, Kim SH, Lee SD, Kim WB, Yang J, Lee MG. Pharmacokinetics of a non-narcotic analgesic, DA-5018, in rats. Biopharm Drug Dispos. 1998 Mar;19(2):101-8. PubMed PMID: 9533110.
4: Shim HJ, Lee JJ, Lee SD, Kim WB, Yang J, Kim SH, Lee MG. Stability, blood partition, and protein binding of DA-5018, a new nonnarcotic analgesic. Res Commun Mol Pathol Pharmacol. 1996 Jan;91(1):97-108. PubMed PMID: 8824935.
5: Cha BJ, Lee ED, Kim WB, Chung SJ, Lee MH, Shim CK. Enhanced skin permeation of a new capsaicin derivative (DA-5018) from a binary vehicle system composed of isopropyl myristate and ethoxydiglycol. Arch Pharm Res. 2001 Jun;24(3):224-8. PubMed PMID: 11440082.
6: Shim HJ, Lee JJ, Lee SD, Kim WB, Yang J, Kim SH, Lee MG. Determination of a new non-narcotic analgesic, DA-5018, in plasma, urine and bile by high-performance liquid chromatography. J Chromatogr B Biomed Sci Appl. 1997 Feb 21;689(2):422-6. PubMed PMID: 9080332.
7: Park YH, You ES, Kim WB, Lee SS. DA-5018, a novel vanilloid type analgesic. Arch Pharm Res. 1997 Feb;20(1):93-5. PubMed PMID: 18975221.
8: Jung J, Hwang SW, Kwak J, Lee SY, Kang CJ, Kim WB, Kim D, Oh U. Capsaicin binds to the intracellular domain of the capsaicin-activated ion channel. J Neurosci. 1999 Jan 15;19(2):529-38. PubMed PMID: 9880573.
9: Shin JS, Wang MH, Hwang SW, Cho H, Cho SY, Kwon MJ, Lee SY, Oh U. Differences in sensitivity of vanilloid receptor 1 transfected to human embryonic kidney cells and capsaicin-activated channels in cultured rat dorsal root ganglion neurons to capsaicin receptor agonists. Neurosci Lett. 2001 Feb 16;299(1-2):135-9. PubMed PMID: 11166956.
10: Pearce LV, Toth A, Ryu H, Kang DW, Choi HK, Jin MK, Lee J, Blumberg PM. Differential modulation of agonist and antagonist structure activity relations for rat TRPV1 by cyclosporin A and other protein phosphatase inhibitors. Naunyn Schmiedebergs Arch Pharmacol. 2008 Apr;377(2):149-57. doi: 10.1007/s00210-007-0258-3. Epub 2008 Feb 8. PubMed PMID: 18259730; PubMed Central PMCID: PMC2931423.
11: Sim JH, Kim YC, Kim SJ, Lee SJ, Suh SH, Jun JY, So I, Kim KW. Capsaicin inhibits the voltage-operated calcium channels intracellularly in the antral circular myocytes of guinea-pig stomach. Life Sci. 2001 Apr 13;68(21):2347-60. PubMed PMID: 11350006.
