Synonym
Articaine HCl; Articaine Hydrochloride; Carticaine HCl; Hoe-40045; Hoe-045; Carticaine Hydrochloride;
IUPAC/Chemical Name
Methyl 4-methyl-3-[2-(propylamino)propanoylamino]thiophene-2-carboxylate Hydrochloride
InChi Key
GDWDBGSWGNEMGJ-UHFFFAOYSA-N
InChi Code
InChI=1S/C13H20N2O3S.ClH/c1-5-6-14-9(3)12(16)15-10-8(2)7-19-11(10)13(17)18-4;/h7,9,14H,5-6H2,1-4H3,(H,15,16);1H
SMILES Code
O=C(C1=C(NC(C(NCCC)C)=O)C(C)=CS1)OC.[H]Cl
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
Biological target:
Articaine hydrochloride (Hoe-045) is used in dental.
In vivo activity:
The evaluation of critical biomarkers has a significant impact on the prognosis of the disease. Therefore, the effect of ART (Articaine) was initially assessed on BUN, CRE, and sCysC, which were known to be characteristic markers for the kidney, and the results are presented in Figure 1. The levels of BUN, CRE, and sCysC were found elevated in the LPS-treated rat group as compared to control, whereas, in the ART-treated group, the level of these biomarkers were found to be significantly decreased in a dose-dependent manner.
Reference: J Biochem Mol Toxicol. 2020 Oct;34(10):e22554. https://pubmed.ncbi.nlm.nih.gov/32687258/
|
Solvent |
mg/mL |
mM |
| Solubility |
| DMSO |
39.5 |
123.12 |
| DMF |
20.0 |
62.34 |
| Ethanol |
34.5 |
107.53 |
| PBS (pH 7.2) |
10.0 |
31.17 |
| Water |
64.0 |
199.48 |
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
320.83
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. Rodrigues da Silva GH, Geronimo G, García-López JP, Ribeiro LNM, de Moura LD, Breitkreitz MC, Feijóo CG, de Paula E. Articaine in functional NLC show improved anesthesia and anti-inflammatory activity in zebrafish. Sci Rep. 2020 Nov 12;10(1):19733. doi: 10.1038/s41598-020-76751-6. PMID: 33184457; PMCID: PMC7665027.
2. Zhao G, Lu S, Li L, Fan X. Local anesthetic articaine ameliorates LPS-induced acute kidney injury via inhibition of NF-ĸB activation and the NLRP3 inflammasome pathway. J Biochem Mol Toxicol. 2020 Oct;34(10):e22554. doi: 10.1002/jbt.22554. Epub 2020 Jul 20. PMID: 32687258.
In vivo protocol:
1. Rodrigues da Silva GH, Geronimo G, García-López JP, Ribeiro LNM, de Moura LD, Breitkreitz MC, Feijóo CG, de Paula E. Articaine in functional NLC show improved anesthesia and anti-inflammatory activity in zebrafish. Sci Rep. 2020 Nov 12;10(1):19733. doi: 10.1038/s41598-020-76751-6. PMID: 33184457; PMCID: PMC7665027.
2. Zhao G, Lu S, Li L, Fan X. Local anesthetic articaine ameliorates LPS-induced acute kidney injury via inhibition of NF-ĸB activation and the NLRP3 inflammasome pathway. J Biochem Mol Toxicol. 2020 Oct;34(10):e22554. doi: 10.1002/jbt.22554. Epub 2020 Jul 20. PMID: 32687258.
1: Shirvani A, Shamszadeh S, Eghbal MJ, Marvasti LA, Asgary S. Effect of preoperative oral analgesics on pulpal anesthesia in patients with irreversible pulpitis-a systematic review and meta-analysis. Clin Oral Investig. 2017 Jan;21(1):43-52. doi: 10.1007/s00784-016-1974-1. Epub 2016 Nov 11. Review. PubMed PMID: 27837343.
2: Yeung V. Articaine--to use or not to use? SAAD Dig. 2016 Jan;32:50-4. Review. PubMed PMID: 27145561.
3: Su N, Li C, Wang H, Shen J, Liu W, Kou L. Efficacy and safety of articaine versus lidocaine for irreversible pulpitis treatment: A systematic review and meta-analysis of randomised controlled trials. Aust Endod J. 2016 Apr;42(1):4-15. doi: 10.1111/aej.12125. Review. PubMed PMID: 27062318.
4: Gazal G, Fareed WM, Zafar MS. Role of intraseptal anesthesia for pain-free dental treatment. Saudi J Anaesth. 2016 Jan-Mar;10(1):81-6. doi: 10.4103/1658-354X.169482. Review. PubMed PMID: 26955316; PubMed Central PMCID: PMC4760049.
5: Bartlett G, Mansoor J. Articaine buccal infiltration vs lidocaine inferior dental block - a review of the literature. Br Dent J. 2016 Feb 12;220(3):117-20. doi: 10.1038/sj.bdj.2016.93. Review. PubMed PMID: 26868800.
6: Kung J, McDonagh M, Sedgley CM. Does Articaine Provide an Advantage over Lidocaine in Patients with Symptomatic Irreversible Pulpitis? A Systematic Review and Meta-analysis. J Endod. 2015 Nov;41(11):1784-94. doi: 10.1016/j.joen.2015.07.001. Epub 2015 Aug 17. Review. PubMed PMID: 26293174.
7: Kakroudi SH, Mehta S, Millar BJ. Articaine hydrochloride: is it the solution? Dent Update. 2015 Jan-Feb;42(1):88-90, 92-3. Review. PubMed PMID: 26062283.
8: Brockmann WG. Mepivacaine: a closer look at its properties and current utility. Gen Dent. 2014 Nov-Dec;62(6):70-5; quiz 76. Review. PubMed PMID: 25369391.
9: Förster JG. Short-acting spinal anesthesia in the ambulatory setting. Curr Opin Anaesthesiol. 2014 Dec;27(6):597-604. doi: 10.1097/ACO.0000000000000126. Review. PubMed PMID: 25211156.
10: Buchwald P, Bodor N. Recent advances in the design and development of soft drugs. Pharmazie. 2014 Jun;69(6):403-13. Review. PubMed PMID: 24974571.
11: Smith T, Urquiola R, Oueis H, Stenger J. Comparison of articaine and lidocaine in the pediatric population. J Mich Dent Assoc. 2014 Jan;96(1):34-7. Review. PubMed PMID: 24654413.
12: Wulf H, Hampl K, Steinfeldt T. Speed spinal anesthesia revisited: new drugs and their clinical effects. Curr Opin Anaesthesiol. 2013 Oct;26(5):613-20. doi: 10.1097/ACO.0b013e3283606b71. Review. PubMed PMID: 26057879.
13: Dou L, Luo J, Yang D, Wang Y. The effectiveness of an additional lingual infiltration in the pulpal anesthesia of mandibular teeth: a systematic review. Quintessence Int. 2013 May;44(5):457-64. doi: 10.3290/j.qi.a29184. Review. PubMed PMID: 23479588.
14: Leith R, Lynch K, O'Connell AC. Articaine use in children: a review. Eur Arch Paediatr Dent. 2012 Dec;13(6):293-6. Review. PubMed PMID: 23235128.
15: Powell V. Articaine is superior to lidocaine in providing pulpal anesthesia. J Am Dent Assoc. 2012 Aug;143(8):897-8. Review. PubMed PMID: 22855904.
16: Becker DE, Reed KL. Local anesthetics: review of pharmacological considerations. Anesth Prog. 2012 Summer;59(2):90-101; quiz 102-3. doi: 10.2344/0003-3006-59.2.90. Review. PubMed PMID: 22822998; PubMed Central PMCID: PMC3403589.
17: Steenen SA, Dubois L, Saeed P, de Lange J. Ophthalmologic complications after intraoral local anesthesia: case report and review of literature. Oral Surg Oral Med Oral Pathol Oral Radiol. 2012 Jun;113(6):e1-5. doi: 10.1016/j.tripleo.2011.07.032. Epub 2012 Feb 18. Review. PubMed PMID: 22677022.
18: Meechan JG. The use of the mandibular infiltration anesthetic technique in adults. J Am Dent Assoc. 2011 Sep;142 Suppl 3:19S-24S. Review. PubMed PMID: 21881058.
19: Förster JG, Rosenberg PH. Revival of old local anesthetics for spinal anesthesia in ambulatory surgery. Curr Opin Anaesthesiol. 2011 Dec;24(6):633-7. doi: 10.1097/ACO.0b013e32834aca1b. Review. PubMed PMID: 21841475.
20: Ogle OE, Mahjoubi G. Advances in local anesthesia in dentistry. Dent Clin North Am. 2011 Jul;55(3):481-99, viii. doi: 10.1016/j.cden.2011.02.007. Review. PubMed PMID: 21726685.
