dihydrotachysterol
Dihydrotachysterol (DHT) is a synthetic vitamin D analog activated in the liver that does not require renal hydroxylation like vitamin D2 (ergocalciferol) and vitamin D3 (cholecalciferol). Dihydrotachysterol is used to treat hypocalcemia, hypoparathyroidism, and prevention of tetany. Dihydrotachysterol is hydroxylated in the liver to 25-hydroxy-dihydrotachysterol, which is the major circulating active form of the drug. Once hydroxylated to 25-hydroxy-dihydrotachysterol, the modified drug binds to the vitamin D receptor. The bound form of the vitamin D receptor serves as a transcriptional regulator of bone matrix proteins, inducing the expression of osteocalcin and suppressing synthesis of type I collagen. Dihydrotachysterol also increases renal phosphate excretion. — NCATS
Clinical trial activity
0 trials · 0 clinical orgs · 0 marketing orgs
Indications
Approved for
Mechanism of action
- Vitamin D receptorAGONIST
VDR agonist
Dihydrotachysterol (DHT) is a synthetic vitamin D analog. Once hydroxylated to 25-hydroxydihydrotachysterol, the modified drug binds to the vitamin D receptor. The bound form of the vitamin D receptor serves as a transcriptional regulator of bone matrix proteins, inducing the expression of osteocalcin and suppressing synthesis of type I collagen. Vitamin D (when bound to the vitamin D receptor)stimulates the expression of a number of proteins involved in transporting calcium from the lumen of the intestine, across the epithelial cells and into blood. This stimulates intestinal calcium absorption and increases renal phosphate excretion.
Chemistry & pharmacology
SMILES
CC(C)[C@@H](C)/C=C/[C@@H](C)[C@H]1CC[C@H]2/C(=C/C=C3\C[C@@H](O)CC[C@@H]3C)CCC[C@]12C- Mol. weight
- 398.68 g/mol
- Lipinski Ro5
- 1 violation(s)
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- ChEMBLCHEMBL2356023 ↗
- WikipediaDihydrotachysterol ↗
- NCATSR5LM3H112R ↗
- ChEMBLCHEMBL2106324 ↗
Also known as
- anti-tetany substance 10
- anti-tetany substance 10
- a.t. 10
- a.t. 10
- dichysterol
- dichysterol
- dichystrolum
- dihidrotaquisterol
- dihidrotaquisterol
- dihydral
- dihydral
- dihydrotachysterol
- dihydrotachysterol
- dihydrotachysterol
- dihydrotachysterol
- dihydrotachysterol
- dihydrotachysterol
- dihydrotachysterol
- dihydrotachysterol
- dihydrotachysterol
- dihydrotachysterolum
- dihydrotachysterolum
- dygratyl
- dygratyl
- hytakerol
- hytakerol
- tachyrol
- tachyrol
- vitamin d1