Calcitriol lactone
Calcitriol lactone (1α,25-Dihydroxyvitamin D3-26,23-lactone) is an endogenous metabolite of vitamin D3. Calcitriol lactone has the biological activity of inhibiting bone resorption and lowering blood calcium. Calcitriol lactone acts as a natural antagonist or partial agonist of VDR by binding to the vitamin D receptor (VDR) and inducing specific conformational changes, thereby regulating the transcription of downstream target genes. Calcitriol lactone can be used in research on bone metabolic diseases (such as osteoporosis) and breast cancer.
For research use only. We do not sell to patients.
- CAS No.: 81203-50-1
- Formula: C27H40O5
- Molecular Weight:444.60
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Endogenous Metabolite Isoforms
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Biological Activity
Description
In Vitro
Calcitriol lactone (1 pM-1 μM; 3 days) is a very weak inhibitor of PHA (HY-N7038)-stimulated human PBMC proliferation, with B50 >1 μM M in DBP-free medium, and no inhibition up to 1 μM in the presence of DBP[4].
Calcitriol lactone (1 h) exhibits weak competitive receptor-binding activity in the prepared cytoplasmic receptor extract from chick intestinal mucosa[2].
Calcitriol lactone binds the cytosolic 1,25-(OH)2D3 receptor, with a relative affinity of 0.5 in HL-60 cells and 0.82 in chicken intestinal cells[4].
Calcitriol lactone (2-10 μM) downregulates nSMase2 in MDA-MB-453, MCF-7, and MDA-MB-231 breast cancer cells without affecting Rab27a expression[7].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wistar (male, weanling, about 100 g at end of 6-week diet period) were fed a vitamin D-deficient and low-calcium diet for 6 weeks[3]
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Dosage:250 ng
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Administration:i.v.; single administration; continuous monitoring for 8, 24, 48, and 96 h
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Result:Stimulated intestinal calcium transport but transiently inhibits and lowers serum calcium levels.
Chemical Information
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CAS No. 81203-50-1
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Molecular Weight 444.60
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Formula C27H40O5
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SMILES
O=C1O[C@@H](C[C@H]([C@H]2CC[C@@]3([H])/C(CCC[C@]23C)=C/C=C4C([C@@H](O)C[C@H](O)C\4)=C)C)C[C@]1(O)C
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Synonyms
1α,25-Dihydroxyvitamin D3-26,23-lactone
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)