P-3298 hemi-fumarate | P3298 | P32/98 | CAS#251572-86-8 | DPP-4 inhibitor

P-3298 hemifumarate
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 530415

CAS#: 251572-86-8 (hemi-fumarate)

Description: P-3298, also known as P32/98, Isoleucine-thiazolidide, is a DPP-4 inhibitor potentially for the treatment of type 2 diabetes. P32/98 decreased non-fasting morning blood glucose more effectively in ZR with iIGT than in ZR with mIGT. Compared with study entry, P32/98 improved DNP of blood glucose in ZR with mIGT and nearly normalized DNP in ZR with iIGT. P32/98 significantly reduced triglycerides and non-esterified fatty acids. Intestinal growth was comparable between inhibitor- and placebo-treated fatty rats.

Chemical Structure

P-3298 hemifumarate

CAS# 251572-86-8 (hemi-fumarate)

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 530415
Name: P-3298 hemifumarate
CAS#: 251572-86-8 (hemi-fumarate)
Chemical Formula: C22H40N4O6S2
Exact Mass: 0.00
Molecular Weight: 520.704
Elemental Analysis: C, 50.75; H, 7.74; N, 10.76; O, 18.44; S, 12.31

Price and Availability

Size	Price	Availability	Quantity
5mg	USD 220
10mg	USD 355
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: P32/98; P-3298; P 3298; P3298; P-3298 hemi-fumarate.

IUPAC/Chemical Name: (2S,3S)-2-amino-3-methyl-1-(thiazolidin-3-yl)pentan-1-one hemifumarate

InChi Key: WEOXCUQGVBLKQX-CXOKTDEKSA-N

InChi Code: InChI=1S/2C9H18N2OS.C4H4O4/c2*1-3-7(2)8(10)9(12)11-4-5-13-6-11;5-3(6)1-2-4(7)8/h2*7-8H,3-6,10H2,1-2H3;1-2H,(H,5,6)(H,7,8)/b;;2-1+/t2*7-,8-;/m00./s1

SMILES Code: CC[C@@H]([C@H](N)C(N1CCSC1)=O)C.O=C(O)/C=C/C(O)=O.CC[C@@H]([C@H](N)C(N2CCSC2)=O)C

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# 136259-20-6 (P 32/98 Free) 251572-86-8 (P 32/98 hemi-fumarate )

Product Data:

Product Data

Instruction:

View handling instruction

Biological target:	P32/98 hemifumarateis a potent inhibitor of dipeptidyl peptidase IV with a Ki value of 130 nM.
In vitro activity:	TBD
In vivo activity:	P32/98 decreased non-fasting morning blood glucose more effectively in ZR with iIGT than in ZR with mIGT. Compared with study entry, P32/98 improved DNP of blood glucose in ZR with mIGT and nearly normalized DNP in ZR with iIGT. An acute bolus of inhibitor reduced glucose load during oGTT in rats chronically treated with placebo or P32/98. In contrast to placebo-treated rats, rats receiving long-term treatment with P32/98 required less insulin during oGTT. This effect was larger in rats with iIGT vs. rats with mIGT. Reference: Diabetes Obes Metab. 2008 Sep;10(10):850-61. https://pubmed.ncbi.nlm.nih.gov/17970756/

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMF	5.0	9.60
	DMSO	15.0	28.81
	Ethanol	1.0	1.92
	PBS (pH 7.2)	10.0	19.20

Preparing Stock Solutions

The following data is based on the product molecular weight 520.70 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. Augstein P, Berg S, Heinke P, Altmann S, Salzsieder E, Demuth HU, Freyse EJ. Efficacy of the dipeptidyl peptidase IV inhibitor isoleucine thiazolidide (P32/98) in fatty Zucker rats with incipient and manifest impaired glucose tolerance. Diabetes Obes Metab. 2008 Sep;10(10):850-61. doi: 10.1111/j.1463-1326.2007.00813.x. Epub 2007 Oct 29. PMID: 17970756. 2. Wargent E, Stocker C, Augstein P, Heinke P, Meyer A, Hoffmann T, Subramanian A, Sennitt MV, Demuth HU, Arch JR, Cawthorne MA. Improvement of glucose tolerance in Zucker diabetic fatty rats by long-term treatment with the dipeptidyl peptidase inhibitor P32/98: comparison with and combination with rosiglitazone. Diabetes Obes Metab. 2005 Mar;7(2):170-81. doi: 10.1111/j.1463-1326.2004.00383.x. PMID: 15715890.
In vitro protocol:	TBD
In vivo protocol:	1. Augstein P, Berg S, Heinke P, Altmann S, Salzsieder E, Demuth HU, Freyse EJ. Efficacy of the dipeptidyl peptidase IV inhibitor isoleucine thiazolidide (P32/98) in fatty Zucker rats with incipient and manifest impaired glucose tolerance. Diabetes Obes Metab. 2008 Sep;10(10):850-61. doi: 10.1111/j.1463-1326.2007.00813.x. Epub 2007 Oct 29. PMID: 17970756. 2. Wargent E, Stocker C, Augstein P, Heinke P, Meyer A, Hoffmann T, Subramanian A, Sennitt MV, Demuth HU, Arch JR, Cawthorne MA. Improvement of glucose tolerance in Zucker diabetic fatty rats by long-term treatment with the dipeptidyl peptidase inhibitor P32/98: comparison with and combination with rosiglitazone. Diabetes Obes Metab. 2005 Mar;7(2):170-81. doi: 10.1111/j.1463-1326.2004.00383.x. PMID: 15715890.

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1: Kushwaha RN, Srivastava R, Mishra A, Rawat AK, Srivastava AK, Haq W, Katti SB. Design, synthesis, biological screening, and molecular docking studies of piperazine-derived constrained inhibitors of DPP-IV for the treatment of type 2 diabetes. Chem Biol Drug Des. 2015 Apr;85(4):439-46. doi: 10.1111/cbdd.12426. PubMed PMID: 25216392.

2: Han B, Huan Y, Lin ZY, Li P, Shen ZF, Yin DL, Huang HH. [Design, synthesis and in vitro activity of glycinamide-bearing compounds as DPP-IV inhibitors]. Yao Xue Xue Bao. 2010 Nov;45(11):1379-84. Chinese. PubMed PMID: 21361038.

3: Yazbeck R, Howarth GS, Geier MS, Demuth HU, Abbott CA. Inhibiting dipeptidyl peptidase activity partially ameliorates colitis in mice. Front Biosci. 2008 May 1;13:6850-8. PubMed PMID: 18508699.

4: Yu BS, Wang AR. Glucagon-like peptide 1 based therapy for type 2 diabetes. World J Pediatr. 2008 Feb;4(1):8-13. doi: 10.1007/s12519-008-0002-1. Review. PubMed PMID: 18402245.

5: Jackson EK, Dubinion JH, Mi Z. Effects of dipeptidyl peptidase iv inhibition on arterial blood pressure. Clin Exp Pharmacol Physiol. 2008 Jan;35(1):29-34. PubMed PMID: 18047624.

6: Augstein P, Berg S, Heinke P, Altmann S, Salzsieder E, Demuth HU, Freyse EJ. Efficacy of the dipeptidyl peptidase IV inhibitor isoleucine thiazolidide (P32/98) in fatty Zucker rats with incipient and manifest impaired glucose tolerance. Diabetes Obes Metab. 2008 Sep;10(10):850-61. PubMed PMID: 17970756.

7: Piteau S, Olver A, Kim SJ, Winter K, Pospisilik JA, Lynn F, Manhart S, Demuth HU, Speck M, Pederson RA, McIntosh CH. Reversal of islet GIP receptor down-regulation and resistance to GIP by reducing hyperglycemia in the Zucker rat. Biochem Biophys Res Commun. 2007 Nov 3;362(4):1007-12. PubMed PMID: 17803965.

8: Jackson EK, Zhang M, Liu W, Mi Z. Inhibition of renal dipeptidyl peptidase IV enhances peptide YY1-36-induced potentiation of angiotensin II-mediated renal vasoconstriction in spontaneously hypertensive rats. J Pharmacol Exp Ther. 2007 Nov;323(2):431-7. PubMed PMID: 17726157.

9: Schlatter P, Beglinger C, Drewe J, Gutmann H. Glucagon-like peptide 1 receptor expression in primary porcine proximal tubular cells. Regul Pept. 2007 Jun 7;141(1-3):120-8. PubMed PMID: 17276524.

10: Wargent E, Stocker C, Augstein P, Heinke P, Meyer A, Hoffmann T, Subramanian A, Sennitt MV, Demuth HU, Arch JR, Cawthorne MA. Improvement of glucose tolerance in Zucker diabetic fatty rats by long-term treatment with the dipeptidyl peptidase inhibitor P32/98: comparison with and combination with rosiglitazone. Diabetes Obes Metab. 2005 Mar;7(2):170-81. PubMed PMID: 15715890.

11: Girardi AC, Knauf F, Demuth HU, Aronson PS. Role of dipeptidyl peptidase IV in regulating activity of Na+/H+ exchanger isoform NHE3 in proximal tubule cells. Am J Physiol Cell Physiol. 2004 Nov;287(5):C1238-45. PubMed PMID: 15213057.

12: Meyer A, Gourinchas E, Girault J, Demuth HU. Quantitative analysis of dipeptidyl peptidase inhibitor P32/98 and its main metabolite in rat, dog, mouse, monkey, human plasma and human urine using liquid chromatography-tandem mass spectrometry: application to pharmacokinetic evaluation. J Chromatogr B Analyt Technol Biomed Life Sci. 2003 Nov 5;796(2):401-11. PubMed PMID: 14581079.

13: Ahrén B. Gut peptides and type 2 diabetes mellitus treatment. Curr Diab Rep. 2003 Oct;3(5):365-72. Review. PubMed PMID: 12975025.

14: Pospisilik JA, Martin J, Doty T, Ehses JA, Pamir N, Lynn FC, Piteau S, Demuth HU, McIntosh CH, Pederson RA. Dipeptidyl peptidase IV inhibitor treatment stimulates beta-cell survival and islet neogenesis in streptozotocin-induced diabetic rats. Diabetes. 2003 Mar;52(3):741-50. PubMed PMID: 12606516.

15: Pospisilik JA, Stafford SG, Demuth HU, McIntosh CH, Pederson RA. Long-term treatment with dipeptidyl peptidase IV inhibitor improves hepatic and peripheral insulin sensitivity in the VDF Zucker rat: a euglycemic-hyperinsulinemic clamp study. Diabetes. 2002 Sep;51(9):2677-83. PubMed PMID: 12196458.

16: Pospisilik JA, Stafford SG, Demuth HU, Brownsey R, Parkhouse W, Finegood DT, McIntosh CH, Pederson RA. Long-term treatment with the dipeptidyl peptidase IV inhibitor P32/98 causes sustained improvements in glucose tolerance, insulin sensitivity, hyperinsulinemia, and beta-cell glucose responsiveness in VDF (fa/fa) Zucker rats. Diabetes. 2002 Apr;51(4):943-50. PubMed PMID: 11916911.

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P-3298 hemifumarate featured