Lobeglitazone Sulfate

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

MedKoo CAT#: 326850

CAS#: 763108-62-9 (Sulfate)

Description: Lobeglitazone, also known as CKD-501, is an antidiabetic drug in the thiazolidinedione class of drugs. As an agonist for both PPARα and PPARγ, it works as an insulin sensitizer by binding to the PPAR receptors in fat cells and making the cells more responsive to insulin.

Chemical Structure

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Lobeglitazone Sulfate
CAS# 763108-62-9 (Sulfate)
Instruction

Theoretical Analysis

MedKoo Cat#: 326850
Name: Lobeglitazone Sulfate
CAS#: 763108-62-9 (Sulfate)
Chemical Formula: C24H26N4O9S2
Exact Mass: 0.00
Molecular Weight: 578.611
Elemental Analysis: C, 49.82; H, 4.53; N, 9.68; O, 24.89; S, 11.08

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

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Related CAS #: 607723-33-1 (free base)   763108-62-9 (Sulfate)    

Synonym: CKD-501; CKD 501; CKD501; Lobeglitazone Sulfate. trade name Duvie, Chong Kun Dang.

IUPAC/Chemical Name: 5-(4-(2-((6-(4-methoxyphenoxy)pyrimidin-4-yl)(methyl)amino)ethoxy)benzyl)thiazolidine-2,4-dione sulfate

InChi Key: IFBYQAMJTBOBHB-UHFFFAOYSA-N

InChi Code: InChI=1S/C24H24N4O5S.H2O4S/c1-28(21-14-22(26-15-25-21)33-19-9-7-17(31-2)8-10-19)11-12-32-18-5-3-16(4-6-18)13-20-23(29)27-24(30)34-20;1-5(2,3)4/h3-10,14-15,20H,11-13H2,1-2H3,(H,27,29,30);(H2,1,2,3,4)

SMILES Code: O=C(N1)SC(CC2=CC=C(OCCN(C3=NC=NC(OC4=CC=C(OC)C=C4)=C3)C)C=C2)C1=O.O=S(O)(O)=O

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# 607723-33-1(Lobeglitazone) 763108-62-9(Lobeglitazone Sulfate)

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 578.61 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:
In vitro protocol:
In vivo protocol:

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1: Kim SH, Kim SG, Kim DM, Woo JT, Jang HC, Chung CH, Ko KS, Park JH, Park YS, Kim SJ, Choi DS. Safety and efficacy of lobeglitazone monotherapy in patients with type 2 diabetes mellitus over 52 weeks: An open-label extension study. Diabetes Res Clin Pract. 2015 Dec;110(3):e27-30. doi: 10.1016/j.diabres.2015.09.009. Epub 2015 Sep 21. PubMed PMID: 26458774.

2: Lim S, Lee KS, Lee JE, Park HS, Kim KM, Moon JH, Choi SH, Park KS, Kim YB, Jang HC. Effect of a new PPAR-gamma agonist, lobeglitazone, on neointimal formation after balloon injury in rats and the development of atherosclerosis. Atherosclerosis. 2015 Nov;243(1):107-19. doi: 10.1016/j.atherosclerosis.2015.08.037. Epub 2015 Sep 4. PubMed PMID: 26363808.

3: Lee JH, Ahn SH, Maeng HJ, Lee W, Kim DD, Chung SJ. The identification of lobeglitazone metabolites in rat liver microsomes and the kinetics of the in vivo formation of the major metabolite M1 in rats. J Pharm Biomed Anal. 2015 Nov 10;115:375-82. doi: 10.1016/j.jpba.2015.07.040. Epub 2015 Jul 30. PubMed PMID: 26275726.

4: Kim CO, Sil Oh E, Kim C, Park MS. Pharmacokinetic Interaction Between Amlodipine and Lobeglitazone, a Novel Peroxisome Proliferator-activated Receptor-γ Agonist, in Healthy Subjects. Clin Ther. 2015 Sep;37(9):1999-2006.e1. doi: 10.1016/j.clinthera.2015.06.009. Epub 2015 Jul 7. PubMed PMID: 26163202.

5: Lee JH, Son JH, Chae YJ, Ahn SH, Lee W, Kim DD, Chung SJ. Gender differences in the hepatic elimination and pharmacokinetics of lobeglitazone in rats. Biopharm Drug Dispos. 2015 Apr 21. doi: 10.1002/bdd.1954. [Epub ahead of print] PubMed PMID: 25899769.

6: Jung JA, Lee SY, Kim TE, Kim JR, Kim C, Huh W, Ko JW. Lack of the effect of lobeglitazone, a peroxisome proliferator-activated receptor-γ agonist, on the pharmacokinetics and pharmacodynamics of warfarin. Drug Des Devel Ther. 2015 Mar 2;9:737-43. doi: 10.2147/DDDT.S76591. eCollection 2015. PubMed PMID: 25767371; PubMed Central PMCID: PMC4354432.

7: Lee JH, Noh CK, Yim CS, Jeong YS, Ahn SH, Lee W, Kim DD, Chung SJ. Kinetics of the Absorption, Distribution, Metabolism, and Excretion of Lobeglitazone, a Novel Activator of Peroxisome Proliferator-Activated Receptor Gamma in Rats. J Pharm Sci. 2015 Sep;104(9):3049-59. doi: 10.1002/jps.24378. Epub 2015 Feb 3. PubMed PMID: 25648999.

8: Jin SM, Park CY, Cho YM, Ku BJ, Ahn CW, Cha BS, Min KW, Sung YA, Baik SH, Lee KW, Yoon KH, Lee MK, Park SW. Lobeglitazone and pioglitazone as add-ons to metformin for patients with type 2 diabetes: a 24-week, multicentre, randomized, double-blind, parallel-group, active-controlled, phase III clinical trial with a 28-week extension. Diabetes Obes Metab. 2015 Jun;17(6):599-602. doi: 10.1111/dom.12435. Epub 2015 Feb 8. PubMed PMID: 25580775.

9: Sil Oh E, Ok Kim C, Kim KH, Kim YN, Kim C, Lee JI, Park MS. Effect of ketoconazole on lobeglitazone pharmacokinetics in Korean volunteers. Clin Ther. 2014 Jul 1;36(7):1064-71. doi: 10.1016/j.clinthera.2014.05.064. Erratum in: Clin Ther. 2014 Oct 1;36(10):1480. PubMed PMID: 25047497.

10: Park MK, Kim TE, Kim J, Kim C, Yoon SH, Cho JY, Jang IJ, Yu KS, Lim KS. Tolerability and pharmacokinetics of lobeglitazone, a novel peroxisome proliferator-activated receptor-γ agonist, after a single oral administration in healthy female subjects. Clin Drug Investig. 2014 Jul;34(7):467-74. doi: 10.1007/s40261-014-0197-y. PubMed PMID: 24802657.

11: Kim SG, Kim DM, Woo JT, Jang HC, Chung CH, Ko KS, Park JH, Park YS, Kim SJ, Choi DS. Efficacy and safety of lobeglitazone monotherapy in patients with type 2 diabetes mellitus over 24-weeks: a multicenter, randomized, double-blind, parallel-group, placebo controlled trial. PLoS One. 2014 Apr 15;9(4):e92843. doi: 10.1371/journal.pone.0092843. eCollection 2014. PubMed PMID: 24736628; PubMed Central PMCID: PMC3988010.

12: Shin D, Kim TE, Yoon SH, Cho JY, Shin SG, Jang IJ, Yu KS. Assessment of the pharmacokinetics of co-administered metformin and lobeglitazone, a thiazolidinedione antihyperglycemic agent, in healthy subjects. Curr Med Res Opin. 2012 Jul;28(7):1213-20. doi: 10.1185/03007995.2012.703131. Epub 2012 Jul 2. PubMed PMID: 22697273.

13: Kim JW, Kim JR, Yi S, Shin KH, Shin HS, Yoon SH, Cho JY, Kim DH, Shin SG, Jang IJ, Yu KS. Tolerability and pharmacokinetics of lobeglitazone (CKD-501), a peroxisome proliferator-activated receptor-γ agonist: a single- and multiple-dose, double-blind, randomized control study in healthy male Korean subjects. Clin Ther. 2011 Nov;33(11):1819-30. doi: 10.1016/j.clinthera.2011.09.023. Epub 2011 Nov 1. PubMed PMID: 22047812.

14: Lee JH, Woo YA, Hwang IC, Kim CY, Kim DD, Shim CK, Chung SJ. Quantification of CKD-501, lobeglitazone, in rat plasma using a liquid-chromatography/tandem mass spectrometry method and its applications to pharmacokinetic studies. J Pharm Biomed Anal. 2009 Dec 5;50(5):872-7. doi: 10.1016/j.jpba.2009.06.003. Epub 2009 Jun 12. PubMed PMID: 19577404.