Sitagliptin 486460-32-6

98.5% up, Medical Grade

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Product Details

Product Information

Product name	Sitagliptin
Molecular Formula	C16H15F6N5O
Molecular Weight	407.32
CAS No.	486460-32-6
Quality Standard	98.9% up, medical grade
Appearance	White powder

COA of Sitagliptin

ITEMS	STANDARDS	RESULTS
Appearance	White or off-white crystalline powder	Complies
Identification	A. Sitagliptin phosphate in water display discriminate reaction of phosphate. B. HPLC: RRT test solution is similar to RRT reference solution. C. IR: Similar to Reference Substance	Complies Complies Complies
Related substance	XG-E ≤0.15%	N.D.
	XG-F ≤0.15%	N.D.
	XG-G ≤0.15%	N.D.
	XG-H ≤0.15%	N.D.
	XG-K ≤0.15%	N.D.
	XG-L ≤0.15%	0.01%
	XG-M ≤0.15%	N.D.
	XG-N ≤0.15%	N.D.
	Other individual impurity ≤0.10%	N.D.
	Total impurities ≤0.5%	0.01%
Isomer	XG-A ≤0.15%	N.D.
Water	3.0%~4.5%	3.6%
Residual solvents	Isopropyl alcohol ≤0.5%	0.02%
	Methyl tert-bytyl ether ≤0.5%	N.D.
	Acetoacetate ≤0.5%	N.D.
	Dimethylformamide ≤0.088%	N.D.
Heavy metals	≤ 10ppm	Complies
Assay	≥98.5% on anhydrous basis	100.3%
Conclusion	Conforms to enterprise standard

Usage

Function of Sitagliptin

Sitagliptin is for dipeptide peptidase 4 (DPP - 4) depressants, by protecting endogenous im fall blood sugar, and enhance its role and control blood sugar levels. Glucose dependence on promoting insulin releasing peptide (GIP) and glucagon peptide 1 (glp-1), as for dietary intake and release of intestinal fall blood sugar.

4 randomized, placebo-controlled trials involving more than 2,000 type 2 diabetes patients evaluated the effect and safety of sitagliptin alone or in combination with other hypoglycemic drugs Sex. The evaluation index is mainly the change value of glycosylated hemoglobin (HbA1c) from the baseline. HbA1c is an indicator of the average blood glucose level in the past 3-4 months. Sitagliptin (100 or 200 mg) alone significantly reduced HbA1c levels. The reduction in HbA1c levels was proportional to the initial level of HbA1c. There was no increase in patient weight during the 24 weeks of single treatment. Sitagliptin reduces fasting and postprandial blood sugar, increases the ratio of preproinsulin/insulin, and improves insulin resistance.

For patients with at least 1500 mg of metformin a day that still cannot control blood sugar well, sitagliptin 100 mg was added. 47% of patients reached the target of HbA1C <7%, while only 18.3% of patients who received placebo achieved the target. Compared with the placebo group, HbA1C in the sitagliptin group decreased by 0.65% on average. The combination of Sitagliptin and metformin has also been shown to be effective as an initial treatment. Patients who were treated with pioglitazone and could not reach the goal (mean HbA1C level was 8.1%) were added sitagliptin 100mg, and the average HbA1C level of patients was reduced by 0.7%. Compared with the pioglitazone alone treatment group, a higher proportion of patients reached HbA1C<7% aims.

*Products under the patent are only for R&D use

Sitagliptin Key Intermediates:

(1) 3-(Trifluoromethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine hydrochloride

CAS No.: 762240-92-6

(2) Boc-(R)-3-Amino-4-(2,4,5-trifluorophenyl)butanoic acid

CAS No.: 486460-00-8