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Semaglutide API Product Description:
COA Available Product with NDC Code

Available in the US and Canada.

Semaglutide API is indicated for improving glycemic control in adults with type 2 diabetes mellitus, in conjunction with diet and exercise. The approved therapeutic doses are 0.5 mg and 1 mg. Type 2 diabetes is a chronic metabolic disorder characterized by high blood sugar, insulin resistance, and insufficient insulin production. The onset of this condition is linked to the inability of beta cells to respond to increased plasma glucose, predominantly caused by lifestyle factors such as overweight and obesity. The key feature of type 2 diabetes is insulin resistance, which reduces insulin’s effectiveness at normal concentrations. Insulin secretion is stimulated by incretins like glucagon-like peptide 1 (GLP-1), which also delays gastric emptying and induces satiety.

Mode of Action:
Semaglutide API enhances glucose control through various mechanisms, including increased insulin secretion, slower gastric emptying, and reduced postprandial glucagon and food intake. The drug mimics the activity of GLP-1, a key hormone in glucose management, thanks to structural modifications that improve its stability against degradation by enzymes like dipeptidyl peptidase-4 (DPP-4). These modifications also promote specific binding to plasma albumin and prevent incorrect binding of fatty acids, resulting in an extended half-life and improved patient compliance.

Pharmacodynamics:
Clinical trials show that semaglutide significantly reduces glycated hemoglobin (HbA1c) compared to other medications, including sitagliptin, exenatide, and insulin glargine U100. HbA1c is a standard measure of high glucose levels, reflecting long-term blood sugar control. Additionally, semaglutide has been shown to reduce body weight, lower fasting and postprandial glucose levels, and decrease fasting triglycerides and VLDL cholesterol.

Metabolism:
Semaglutide is slowly but extensively metabolized before excretion, with 83% of the administered dose found unchanged in plasma. Six different metabolites have been identified, with the major metabolite accounting for 7.7% of the dose. The drug is primarily degraded by enzymes such as DPP-4 and neural endopeptidase (NEP), which inactivate semaglutide and hydrolyze its peptide bonds.

Toxicity:
In preclinical studies, mild c-cell hyperplasia and other effects, including liver necrosis and centrilobular hypertrophy, were observed at doses significantly higher than those used clinically. High doses also resulted in ECG abnormalities and tissue vacuolation.

IUPAC:
17-{[(1R)-3-[(2-{2-[({2-[2-({[(5S)-5-[(2S)-2-[(2S)-2-[(2S)-2-{2-[(2S)-2-[(2S)-2-[(2S)-2-[(2S)-2-[(2S)-2-[(2S)-2-[(2S)-2-[(2S)-2-[(2S,3R)-2-[(2S)-2-[(2S,3R)-2-{2-[(2S)-2-{2-[(2S)-2-amino-3-(1H-imidazol-4-yl)propanamido]-2-methylpropanamido}-4-carboxybutanamido]acetamido}-3-hydroxybutanamido]-3-phenylpropanamido]-3-hydroxybutanamido]-3-hydroxypropanamido]-3-carboxypropanamido]-3-methylbutanamido]-3-hydroxypropanamido]-3-hydroxypropanamido]-3-(4-hydroxyphenyl)propanamido]-4-methylpentanamido]-4-carboxybutanamido]acetamido}-4-carbamoylbutanamido]propanamido]propanamido]-5-{[(1S)-1-{[(1S)-1-{[(1S,2S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-4-carbamimidamido-1-[({[(1S)-4-carbamimidamido-1-[(carboxymethyl)carbamoyl]butyl]carbamoyl}methyl)carbamoyl]butyl]carbamoyl}-2-methylpropyl]carbamoyl}-3-methylbutyl]carbamoyl}-2-(1H-indol-3-yl)ethyl]carbamoyl}ethyl]carbamoyl}-2-methylbutyl]carbamoyl}-2-phenylethyl]carbamoyl}-3-carboxypropyl]carbamoyl}pentyl]carbamoyl}methoxy)ethoxy]ethyl}carbamoyl)methoxy]ethoxy}ethyl)carbamoyl]-1-carboxypropyl]carbamoyl}heptadecanoic acid

DrugBank:
DB13928

Formula:
C187-H291-N45-O59

Molecular Mass:
Average: 4113.641
Monoisotopic: 4111.11537713

Synonyms:
Semaglutide / Semaglutide API
SMILES:
CC[C@H](C)[C@H](NC(=O)[C@H](CC1=CC=CC=C1)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCCCNC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@@H](NC(=O)CCCCCCCCCCCCCCCCC(O)=O)C(O)=O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC1=CC=C(O)C=C1)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC1=CC=CC=C1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)C(C)(C)NC(=O)[C@@H](N)CC1=CNC=N1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC1=CNC2=C1C=CC=C2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)NCC(=O)N[C@@H](CCCNC(N)=N)C(=O)NCC(O)=O
InChi:
InChI=1S/C187H291N45O59/c1-18-105(10)154(180(282)208-108(13)159(261)216-133(86-114-89-200-119-50-40-39-49-117(114)119)170(272)218-129(82-102(4)5)171(273)228-152(103(6)7)178(280)215-121(53-44-72-199-186(192)193)162(264)201-91-141(242)209-120(52-43-71-198-185(190)191)161(263)204-94-151(257)258)230-172(274)131(83-111-45-33-31-34-46-111)219-167(269)126(64-69-149(253)254)214-166(268)122(51-41-42-70-195-144(245)98-290-79-78-289-76-74-197-145(246)99-291-80-77-288-75-73-196-139(240)66-61-127(183(285)286)211-140(241)54-37-29-27-25-23-21-19-20-22-24-26-28-30-38-55-146(247)248)212-158(260)107(12)206-157(259)106(11)207-165(267)125(60-65-138(189)239)210-142(243)92-202-163(265)123(62-67-147(249)250)213-168(270)128(81-101(2)3)217-169(271)130(85-113-56-58-116(238)59-57-113)220-175(277)135(95-233)223-177(279)137(97-235)224-179(281)153(104(8)9)229-174(276)134(88-150(255)256)221-176(278)136(96-234)225-182(284)156(110(15)237)231-173(275)132(84-112-47-35-32-36-48-112)222-181(283)155(109(14)236)227-143(244)93-203-164(266)124(63-68-148(251)252)226-184(287)187(16,17)232-160(262)118(188)87-115-90-194-100-205-115/h31-36,39-40,45-50,56-59,89-90,100-110,118,120-137,152-156,200,233-238H,18-30,37-38,41-44,51-55,60-88,91-99,188H2,1-17H3,(H2,189,239)(H,194,205)(H,195,245)(H,196,240)(H,197,246)(H,201,264)(H,202,265)(H,203,266)(H,204,263)(H,206,259)(H,207,267)(H,208,282)(H,209,242)(H,210,243)(H,211,241)(H,212,260)(H,213,270)(H,214,268)(H,215,280)(H,216,261)(H,217,271)(H,218,272)(H,219,269)(H,220,277)(H,221,278)(H,222,283)(H,223,279)(H,224,281)(H,225,284)(H,226,287)(H,227,244)(H,228,273)(H,229,276)(H,230,274)(H,231,275)(H,232,262)(H,247,248)(H,249,250)(H,251,252)(H,253,254)(H,255,256)(H,257,258)(H,285,286)(H4,190,191,198)(H4,192,193,199)/t105-,106-,107-,108-,109 ,110 ,118-,120-,121-,122-,123-,124-,125-,126-,127 ,128-,129-,130-,131-,132-,133-,134-,135-,136-,137-,152-,153-,154-,155-,156-/m0/s1

Purchase of this product is restricted to licensed companies and labs.

ProActive Self Adhesive Electrode is a versatile and reusable electrode that can be used with most TENS and muscle electro stimulators. With a built-in conductive gel surface that remains effective for up to 30 uses,ProActive Self Adhesive Electrode is pre-wired and pre-gelled for easy and convenient application. The flexible cloth backing allows the electrode to conform to all body surfaces, while the rounded edges prevent electrode curl-up. The hypo-allergenic gel keeps the skin soft and the anchored pigtail prevents wire pull-out, increasing the usage life. Available in a variety of shapes and sizes, these latex-free electrodes are perfect for multiple treatment zones.

Self-adhesive, pre-gelled & reusable Electrodes for use with most TENS and muscle electro stimulators

• Built-in conductive gel surface remains effective for up to 30 uses
• Flexible cloth backing allows the electrode to easily and durably conform to all body surfaces
• Pre-wired and pre-gelled for easy and convenient application
• Long lasting, hypo-allergenic gel keeps skin soft
• Rounded edges for prevention of electrode curl-up
• Anchored pigtail prevents wire pull-out and increases usage life
• Available in a variety of shapes and sizes for application to multiple treatment zones
• Latex-Free