Home / Products / Orforglipron Hemicalcium Hydrate
Building Blocks CAS 3008544-96-2 Featured

Orforglipron Hemicalcium Hydrate

Orforglipron hemicalcium hydrate (development codes LY3502970/OWL-833) is the world's first oral, non-peptide small-molecule GLP-1 receptor agonist to complete Phase III trials and receive marketing approval. It binds allosterically to the transmembrane pocket of the GLP-1 receptor via a rigid polycyclic heteroaromatic scaffold (Ki ≈ 1 nM), shows biased agonism toward the cAMP pathway with almost no β-arrestin recruitment, contains no peptide bonds, and is not degraded by proteases such as DPP-4; it can therefore be taken orally once daily without food or water restrictions. This product is the hemicalcium salt monohydrate, in which 2 molecules of orforglipron free acid form a salt with 1 calcium ion together with water of crystallization; it is a white to off-white crystalline powder with HPLC purity ≥99.0%, complying with CHP/USP/EP standards, and is used for the development and CMO contract manufacturing of oral solid dosage forms for type 2 diabetes and obesity.

Product Overview

Orforglipron (LY3502970/OWL-833) is an oral non-peptide small-molecule GLP-1 receptor agonist developed by Eli Lilly. Its scaffold centers on a 4-methyl-tetrahydropyrazolo[4,3-c]pyridine core, linked via an amide bond to an indole fragment bearing a (4S)-2,2-dimethyltetrahydropyran-4-yl group and an N-substituted 2-methylcyclopropyl-1,2,4-oxadiazolone; the molecule contains no peptide bonds at all, is resistant to gastrointestinal enzymatic hydrolysis and gastric acid, and is orally absorbed without the need for absorption enhancers. In the marketed formulation, the oxadiazolone exists as the deprotonated calcium salt (hemicalcium salt).

This product is the hemicalcium salt monohydrate of that active ingredient: 2 molecules of orforglipron weak acid form a 2:1 salt with 1 Ca²⁺ ion, together with 1 molecule of water of crystallization. Compared with the free acid and the sodium salt, the hemicalcium salt has a more stable crystal form, lower hygroscopicity, and better dissolution and oral bioavailability; it is suitable for wet granulation and tableting processes and does not readily lose water or undergo crystal form conversion during routine formulation processing.

Technical Specifications

  • Standards: CHP/USP/EP
  • Specification: 0.99 (purity ≥99.0%, HPLC)
  • CAS Number: 3008544-96-2
  • Molecular Formula: C₄₈H₄₈F₂N₁₀O₅·½Ca·H₂O (hemicalcium salt monohydrate); calculated as the 2:1:2 bimolecular salt form, C₉₆H₉₈CaF₄N₂₀O₁₂ (PubChem UNII UV478AZB7Z)
  • Molecular Weight: 921.02 g/mol (hemicalcium salt monohydrate); approximately 1840.0 g/mol calculated as the 2:1:2 bimolecular salt form (PubChem calculated value)
  • Appearance: White to off-white crystalline powder (the FDA prescribing information describes the API as a white to off-white/light brown, hygroscopic solid)
  • Purity (HPLC): ≥ 99.0%
  • Melting Point: No official melting point recorded in publicly available CHP/USP/EP, FDA, or EMA materials; some suppliers’ COAs state 268–275 °C, which is single-source data for reference only and not a release specification
  • Chemical Name: Calcium 3-((1S,2S)-1-(5-((S)-2,2-dimethyltetrahydro-2H-pyran-4-yl)-2-((S)-3-(3-(4-fluoro-1-methyl-1H-indazol-5-yl)-2-oxo-2,3-dihydro-1H-imidazol-1-yl)-2-(4-fluoro-3,5-dimethylphenyl)-4-methyl-4,5,6,7-tetrahydro-2H-pyrazolo[4,3-c]pyridine-5-carbonyl)-1H-indol-1-yl)-2-methylcyclopropyl)-1,2,4-oxadiazol-5(4H)-one hydrate (2:1:2)
  • Chiral Centers: Fixed (1S,2S) and (4S) configurations
  • Solubility: Freely soluble in DMSO (about 25–50 mg/mL, sonication required; water-absorbed DMSO markedly reduces solubility), DMF, dichloromethane, and THF; slightly soluble/soluble in methanol and ethanol; practically insoluble in water
  • Calcium Content: 1.8%–2.5% (1.8%–2.4% calculated on the anhydrous basis)
  • Water Content: 3.0%–7.0% (slight variation among enterprise standards; typical batches about 5.3%)
  • Related Substances: Single impurity ≤0.10%–0.2%, total impurities ≤1.0%; enantiomer ≤0.10%
  • Assay (HPLC, anhydrous basis): 98.0%–102.0%
  • Storage: Seal tightly at 4 °C (2–8 °C), protect from light and moisture; long-term storage at −20 °C is acceptable; solutions should be aliquoted and stored at −80 °C, avoiding repeated freeze-thaw cycles

Applications

  • Long-term weight management (obesity/overweight): On April 1, 2026, the US FDA approved Foundayo (orforglipron) tablets, as an adjunct to a reduced-calorie diet and increased physical activity, for weight reduction and long-term maintenance in adults with obesity, or overweight adults with at least one weight-related comorbidity; starting dose 0.8 mg once daily, escalating to 2.5 mg after at least 30 days and to 5.5 mg after a further 30 days, with further increases to 9 mg, 14.5 mg, and 17.2 mg based on efficacy and tolerability; dosing is not restricted by food or water intake
  • Type 2 diabetes mellitus (T2DM): The pivotal Phase III ATTAIN-2 study demonstrated significant weight reduction and improvement of metabolic parameters including HbA1c in a T2DM population with overweight/obesity; regulatory review for this indication is still ongoing (an EMA committee has issued positive opinions for obesity and type 2 diabetes, and a marketing application has been submitted in China); refer to the latest official announcements for formal approval status
  • Mechanism research: Glucose-dependent enhancement of insulin secretion and suppression of glucagon release; delayed gastric emptying and action on central appetite-regulation pathways to reduce caloric intake; used for GLP-1R binding assays, cAMP-biased signaling studies, and in vitro and in vivo pharmacodynamic/pharmacokinetic evaluation
  • Formulation and manufacturing: Suitable for formulation development of oral solid dosage forms such as tablets and capsules, crystal form and salt form screening, impurity reference standards, and stability studies; can serve as a pharmaceutical intermediate/API for GMP scale-up and CMO/CDMO contract manufacturing

Safety Notice: This product is a pharmaceutical active ingredient/pharmaceutical intermediate intended solely for compliant research and pharmaceutical manufacturing use; it is not intended for end clinical use or self-medication guidance. The marketed formulation label carries a boxed warning for thyroid C-cell tumors; it is contraindicated in patients with a personal or family history of medullary thyroid carcinoma or in patients with multiple endocrine neoplasia syndrome type 2 (MEN 2).

Product information: please contact us. This information is for reference only.

Need a quotation or sample?

Tell us your required quantity, purity grade and destination. Our team will respond within 24 hours.

Request a Quote →

Related Products

Building Blocks CAS 185104-11-4

Acotiamide Hydrochloride

Acotiamide Hydrochloride (development codes YM-443／Z-338, brand name Acofide) is the world's first orally administered gastroprokinetic drug approved for functional dyspepsia (FD), and belongs to the thiazolecarboxamide class of compounds. It is a novel, orally active, selective, reversible acetylcholinesterase (AChE) inhibitor — by inhibiting AChE it reduces acetylcholine degradation and increases acetylcholine concentration in the synaptic cleft, thereby enhancing antral and gastric body contractility, improving delayed gastric emptying, and promoting gastric accommodation. It is used for symptoms of functional dyspepsia such as postprandial fullness, upper abdominal bloating, and early satiation. This product is a white to off-white crystalline powder with purity ≥99.0%, manufactured to CHP／USP／EP standards.

View product →
Building Blocks CAS 1415456-99-3 / 910463-68-2

Cagrilintide + Semaglutide (CagriSema)

CagriSema is a fixed-dose combination injectable of the long-acting amylin analogue cagrilintide and the GLP-1 receptor agonist semaglutide, achieving synergistic weight loss through the complementary mechanisms of "reducing hunger + enhancing satiety". Cagrilintide is a 37-amino-acid acylated amylin analogue and a non-selective agonist of amylin receptors (AMYR) and the calcitonin G protein-coupled receptor (CTR); semaglutide is a GLP-1 analogue that promotes insulin secretion and suppresses glucagon in a glucose-dependent manner. Both are white to off-white lyophilized powders with HPLC purity ≥99.0%, manufactured to CHP／USP／EP standards, for the development and CMO contract manufacturing of injectables for long-term weight management in obesity/overweight and for type 2 diabetes.

View product →
Building Blocks CAS 32222-06-3

Calcitriol

Calcitriol (i.e., 1α,25-dihydroxyvitamin D₃, 1,25-(OH)₂D₃, brand names Rocaltrol, Calcijex) is the **naturally active form** of vitamin D₃ produced in the body through hepatic 25-hydroxylation and renal 1α-hydroxylation, and is the most potent known vitamin D₃ metabolite. As the natural ligand of the vitamin D receptor (VDR), it acts mainly on the intestine and bone, promoting intestinal calcium and phosphate absorption, mobilizing bone calcium, and working with PTH to regulate calcium-phosphate homeostasis, while suppressing parathyroid PTH secretion. It is used for renal osteodystrophy and hypocalcemia in chronic renal failure (especially in dialysis patients), hypoparathyroidism, rickets/osteomalacia, and postmenopausal osteoporosis. This product is a white to off-white crystalline powder, **sensitive to air and light**, with purity ≥99.0%, manufactured to CHP／USP／EP standards.

View product →