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MedKoo Cat#: 326800 | Name: Mitiglinide calcium
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Description:

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

Mitiglinide calcium is a Potassiun Channel blocker. Mitiglinide is thought to stimulate insulin secretion by closing the ATP-sensitive K(+) K(ATP) channels in pancreatic beta-cells. Mitiglinide may be potential useful for the treatment of type 2 diabetes. Mitiglinide belongs to the meglitinide class of blood glucose-lowering drugs.

Chemical Structure

Mitiglinide calcium
Mitiglinide calcium
CAS#145525-41-3 (calcium)

Theoretical Analysis

MedKoo Cat#: 326800

Name: Mitiglinide calcium

CAS#: 145525-41-3 (calcium)

Chemical Formula: C38H48CaN2O6

Exact Mass: 0.0000

Molecular Weight: 334.44

Elemental Analysis: C, 68.24; H, 7.23; Ca, 5.99; N, 4.19; O, 14.35

Price and Availability

Size Price Availability Quantity
100mg USD 250.00 2 weeks
250mg USD 450.00 2 weeks
1g USD 950.00 2 Weeks
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Related CAS #
No Data
Synonym
KAD-1229; KAD 1229; KAD1229; S 21403; Mitiglinide calcium; Glufast.
IUPAC/Chemical Name
calcium 2-benzyl-4-((3aR,7aS)-octahydro-2H-isoindol-2-yl)-4-oxobutanoate
InChi Key
PMRVFZXOCRHXFE-RJAPBONKSA-L
InChi Code
InChI=1S/2C19H25NO3.Ca/c2*21-18(20-12-15-8-4-5-9-16(15)13-20)11-17(19(22)23)10-14-6-2-1-3-7-14;/h2*1-3,6-7,15-17H,4-5,8-13H2,(H,22,23);/q;;+2/p-2/t2*15-,16+,17?;
SMILES Code
O=C([O-])C(CC1=CC=CC=C1)CC(N2C[C@]3([H])CCCC[C@]3([H])C2)=O.O=C([O-])C(CC4=CC=CC=C4)CC(N5C[C@]6([H])CCCC[C@]6([H])C5)=O.[Ca+2]
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
Related CAS# CAS#145375-43-5 (Mitiglinide free acid). CAS#145525-41-3 (Mitiglinide calcium) CAS#207844-01-7 (Mitiglinide calcium dihydrate)
Product Data
Product Data
Instruction
View handling instruction
Biological target:
Mitiglinide Calcium (KAD-1229 anhydrous), an insulinotropic agent, is an ATP-sensitive K+ (KATP) channel antagonist.
In vitro activity:
Kir6.2 was coexpressed with SUR1, SUR2A or SUR2B in Xenopus oocytes and macroscopic currents were recorded in giant inside-out membrane patches. Mitiglinide was added to the intracellular membrane surface. Mitiglinide inhibited Kir6.2/SUR currents at two sites: a low-affinity site on Kir6.2 and a high-affinity site on SUR. Reference: Br J Pharmacol. 2001 Apr;132(7):1542-8. https://pubmed.ncbi.nlm.nih.gov/11264248/
In vivo activity:
The effects of KAD-1229 (a novel non-sulphonylurea agent), voglibose (an alpha-glucosidase inhibitor) and nateglinide (a non-sulphonylurea antihyperglycaemic agent) on hyperglycaemia induced by a meal load were assessed in diabetic rats. KAD-1229 suppressed the increase in plasma glucose levels seen after a meal load and the area under the curve for plasma glucose levels (AUCglucose) up to 5 h after the meal load. Reference: Clin Exp Pharmacol Physiol. 2002 May-Jun;29(5-6):423-7. https://pubmed.ncbi.nlm.nih.gov/12010187/
Solvent mg/mL mM comments
Solubility
DMSO 5.0 14.95
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 334.44 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:
1. Reimann F, Proks P, Ashcroft FM. Effects of mitiglinide (S 21403) on Kir6.2/SUR1, Kir6.2/SUR2A and Kir6.2/SUR2B types of ATP-sensitive potassium channel. Br J Pharmacol. 2001 Apr;132(7):1542-8. doi: 10.1038/sj.bjp.0703962. Erratum in: Br J Pharmacol. 2011 Apr;162(8):1894. PMID: 11264248; PMCID: PMC1572697. 2. Sunaga Y, Gonoi T, Shibasaki T, Ichikawa K, Kusama H, Yano H, Seino S. The effects of mitiglinide (KAD-1229), a new anti-diabetic drug, on ATP-sensitive K+ channels and insulin secretion: comparison with the sulfonylureas and nateglinide. Eur J Pharmacol. 2001 Nov 9;431(1):119-25. doi: 10.1016/s0014-2999(01)01412-1. PMID: 11716850. 3. Ichikawa K, Yamato T, Ojima K, Tsuji A, Ishikawa K, Kusama H, Kojima M. Effect of KAD-1229, a novel hypoglycaemic agent, on plasma glucose levels after meal load in type 2 diabetic rats. Clin Exp Pharmacol Physiol. 2002 May-Jun;29(5-6):423-7. doi: 10.1046/j.1440-1681.2002.03682.x. PMID: 12010187. 4. Ohnota H, Kitamura T, Kinukawa M, Hamano S, Shibata N, Miyata H, Ujiie A. A rapid- and short-acting hypoglycemic agent KAD-1229 improves post-prandial hyperglycemia and diabetic complications in streptozotocin-induced non-insulin-dependent diabetes mellitus rats. Jpn J Pharmacol. 1996 Aug;71(4):315-23. doi: 10.1254/jjp.71.315. PMID: 8886929.
In vitro protocol:
1. Reimann F, Proks P, Ashcroft FM. Effects of mitiglinide (S 21403) on Kir6.2/SUR1, Kir6.2/SUR2A and Kir6.2/SUR2B types of ATP-sensitive potassium channel. Br J Pharmacol. 2001 Apr;132(7):1542-8. doi: 10.1038/sj.bjp.0703962. Erratum in: Br J Pharmacol. 2011 Apr;162(8):1894. PMID: 11264248; PMCID: PMC1572697. 2. Sunaga Y, Gonoi T, Shibasaki T, Ichikawa K, Kusama H, Yano H, Seino S. The effects of mitiglinide (KAD-1229), a new anti-diabetic drug, on ATP-sensitive K+ channels and insulin secretion: comparison with the sulfonylureas and nateglinide. Eur J Pharmacol. 2001 Nov 9;431(1):119-25. doi: 10.1016/s0014-2999(01)01412-1. PMID: 11716850.
In vivo protocol:
1. Ichikawa K, Yamato T, Ojima K, Tsuji A, Ishikawa K, Kusama H, Kojima M. Effect of KAD-1229, a novel hypoglycaemic agent, on plasma glucose levels after meal load in type 2 diabetic rats. Clin Exp Pharmacol Physiol. 2002 May-Jun;29(5-6):423-7. doi: 10.1046/j.1440-1681.2002.03682.x. PMID: 12010187. 2. Ohnota H, Kitamura T, Kinukawa M, Hamano S, Shibata N, Miyata H, Ujiie A. A rapid- and short-acting hypoglycemic agent KAD-1229 improves post-prandial hyperglycemia and diabetic complications in streptozotocin-induced non-insulin-dependent diabetes mellitus rats. Jpn J Pharmacol. 1996 Aug;71(4):315-23. doi: 10.1254/jjp.71.315. PMID: 8886929.
1: Son JW, Lee IK, Woo JT, Baik SH, Jang HC, Lee KW, Cha BS, Sung YA, Park TS, Yoo SJ, Yoon KH. A prospective, randomized, multicenter trial comparing the efficacy and safety of the concurrent use of long-acting insulin with mitiglinide or voglibose in patients with type 2 diabetes. Endocr J. 2015;62(12):1049-57. doi: 10.1507/endocrj.EJ15-0325. Epub 2015 Sep 25. PubMed PMID: 26411328. 2: Takeshita Y, Takamura T, Kita Y, Takazakura A, Kato K, Isobe Y, Kaneko S. Sitagliptin versus mitiglinide switched from mealtime dosing of a rapid-acting insulin analog in patients with type 2 diabetes: a randomized, parallel-group study. BMJ Open Diabetes Res Care. 2015 Aug 28;3(1):e000122. doi: 10.1136/bmjdrc-2015-000122. eCollection 2015. PubMed PMID: 26336611; PubMed Central PMCID: PMC4553908. 3: Al Azzam KM, Muhammad E. Host-guest Inclusion Complexes between Mitiglinide and the Naturally Occurring Cyclodextrins α, β, and γ: A Theoretical Approach. Adv Pharm Bull. 2015 Jun;5(2):289-91. doi: 10.15171/apb.2015.040. Epub 2015 Jun 1. PubMed PMID: 26236670; PubMed Central PMCID: PMC4517090. 4: Tani S, Nagao K, Hirayama A. Differences between Mitiglinide/Voglibose Fixed-dose Combination and Glimepiride in Modifying Low-density Lipoprotein Heterogeneity in Japanese Type-2 Diabetic Patients: A Pilot Study. Drug Res (Stuttg). 2016 Feb;66(2):94-9. doi: 10.1055/s-0035-1549993. Epub 2015 May 26. PubMed PMID: 26011816. 5: Baek JH, Jin SM, Kaku K, Jung JA, Kim JR, Ko JW, Kim MJ, Lee SY, Huh WS, Kim JH. Efficacy of mitiglinide and sitagliptin, alone or in combination, on postprandial excursion and glycemic variability assessed by continuous glucose monitoring: a post hoc analysis with single-day treatment. Expert Opin Pharmacother. 2015 Jun;16(8):1127-36. doi: 10.1517/14656566.2015.1035646. Epub 2015 Apr 16. PubMed PMID: 25881690. 6: Murakami T, Nambu T, Kato T, Matsuda Y, Yonemitsu S, Muro S, Oki S. Add-on treatment with mitiglinide improves residual postprandial hyperglycemia in type 2 diabetic patients receiving the combination therapy with insulin glargine and sitagliptin. Tohoku J Exp Med. 2015;235(4):255-60. doi: 10.1620/tjem.235.255. PubMed PMID: 25810423. 7: Ando K, Nishimura R, Seo C, Tsujino D, Sakamoto M, Utsunomiya K. Comparing postprandial efficacy in type 2 diabetic patients receiving mitiglinide and sitagliptin by using continuous glucose monitoring: a pilot study. Expert Opin Pharmacother. 2014 Dec;15(17):2479-85. doi: 10.1517/14656566.2014.970531. Epub 2014 Oct 20. PubMed PMID: 25327311. 8: Akahane K, Inoue T, Yokoyama A, Yaguchi A, Ojima K, Kiguchi S, Maruyama K, Kobayashi M, Mori Y. Efficacy of Mitiglinide Combined with Dapagliflozin in Streptozotocin-nicotinamide-induced Type 2 Diabetic Rats and in Zucker Fatty Rats. Drug Res (Stuttg). 2015 Aug;65(8):416-21. doi: 10.1055/s-0034-1387719. Epub 2014 Sep 4. PubMed PMID: 25188606. 9: Ono Y, Kamoshima H, Nakamura A, Nomoto H. Glycemic/metabolic responses to identical meal tolerance tests at breakfast, lunch and dinner in Japanese patients with type 2 diabetes mellitus treated with a dipeptidyl peptidase-4 inhibitor and the effects of adding a mitiglinide/voglibose fixed-dose combination. Expert Opin Pharmacother. 2014 Sep;15(13):1785-95. doi: 10.1517/14656566.2014.939070. Epub 2014 Jul 21. PubMed PMID: 25046055. 10: Osonoi T, Saito M, Tamasawa A, Ishida H, Osonoi Y. Effects of sitagliptin or mitiglinide as an add-on to acarbose on daily blood glucose fluctuations measured by 72 h subcutaneous continuous glucose monitoring in Japanese patients with type 2 diabetes: a prospective randomized study. Expert Opin Pharmacother. 2014 Jul;15(10):1325-35. doi: 10.1517/14656566.2014.920323. Epub 2014 May 27. Erratum in: Expert Opin Pharmacother. 2014 Aug;15(11):1637. PubMed PMID: 24866329. 11: Kimura H, Matsuda H, Fujimoto H, Arimitsu K, Toyoda K, Mukai E, Nakamura H, Ogawa Y, Takagi M, Ono M, Inagaki N, Saji H. Synthesis and evaluation of 18F-labeled mitiglinide derivatives as positron emission tomography tracers for β-cell imaging. Bioorg Med Chem. 2014 Jul 1;22(13):3270-8. doi: 10.1016/j.bmc.2014.04.059. Epub 2014 May 6. PubMed PMID: 24842616. 12: Ihana N, Tsujimoto T, Yamamoto-Honda R, Kishimoto M, Kajio H, Noto H, Kakei M, Noda M. Improvement of both fasting and postprandial glycemic control by the two-step addition of miglitol and mitiglinide to basal insulin therapy: a pilot study. Diabetol Metab Syndr. 2014 Mar 31;6:48. doi: 10.1186/1758-5996-6-48. eCollection 2014. PubMed PMID: 24684803; PubMed Central PMCID: PMC4025538. 13: Kaku K, Inagaki N, Kobayashi N. Long-term Effects of Mitiglinide in Japanese Diabetics Inadequately Controlled with DPP-4 Inhibitor or Biguanide Monotherapy. Diabetes Ther. 2014 Jun;5(1):97-111. doi: 10.1007/s13300-014-0051-5. Epub 2014 Feb 1. PubMed PMID: 24488695; PubMed Central PMCID: PMC4065298. 14: Zeng Y, Xie X, Duan J, Zhou T, Zhang Y, Yang M, Xu F. Perturbation of mitiglinide metabolism by chronic unpredicted mild stress in rats. Sci Rep. 2014 Jan 21;4:3794. doi: 10.1038/srep03794. PubMed PMID: 24445843; PubMed Central PMCID: PMC3896903. 15: Ono Y, Nakamura A, Cho KY, Nomoto H. The glycemic/metabolic responses to meal tolerance tests at breakfast, lunch and dinner, and effects of the mitiglinide/voglibose fixed-dose combination on postprandial profiles in Japanese patients with type 2 diabetes mellitus. Expert Opin Pharmacother. 2014 Feb;15(3):311-24. doi: 10.1517/14656566.2014.868437. Epub 2013 Dec 13. PubMed PMID: 24328511. 16: Jung JA, Kaku K, Kim JH, Kim JR, Ko JW, Lee SY, Huh W. Additive postprandial glucose-lowering effects of mitiglinide and sitagliptin in patients with type 2 diabetes mellitus. Adv Ther. 2013 Nov;30(11):1018-29. doi: 10.1007/s12325-013-0072-x. Epub 2013 Nov 19. Erratum in: Adv Ther. 2014 Jan;31(1):149. PubMed PMID: 24249434. 17: Ohta A, Ohshige T, Sakai K, Nakamura Y, Tenjin A, Tsukiyama S, Terashima Y, Matsubara F, Kawata T, Nagai Y, Tanaka Y. Comparison of the hypoglycemic effect of sitagliptin versus the combination of mitiglinide and voglibose in drug-naïve Japanese patients with type 2 diabetes. Expert Opin Pharmacother. 2013 Dec;14(17):2315-22. doi: 10.1517/14656566.2013.842554. Epub 2013 Sep 30. PubMed PMID: 24079645. 18: Konya H, Katsuno T, Tsunoda T, Yano Y, Kamitani M, Miuchi M, Hamaguchi T, Miyagawa J, Namba M. Effects of combination therapy with mitiglinide and voglibose on postprandial plasma glucose in patients with type 2 diabetes mellitus. Diabetes Metab Syndr Obes. 2013 Sep 2;6:317-25. doi: 10.2147/DMSO.S36046. Review. PubMed PMID: 24039439; PubMed Central PMCID: PMC3769413. 19: Phillippe HM, Wargo KA. Mitiglinide for type 2 diabetes treatment. Expert Opin Pharmacother. 2013 Oct;14(15):2133-44. doi: 10.1517/14656566.2013.834048. Epub 2013 Aug 30. Review. PubMed PMID: 23992284. 20: Kodani N, Saisho Y, Tanaka K, Kawai T, Itoh H. Effects of mitiglinide, a short-acting insulin secretagogue, on daily glycemic variability and oxidative stress markers in Japanese patients with type 2 diabetes mellitus. Clin Drug Investig. 2013 Aug;33(8):563-70. PubMed PMID: 23797928.