Lexacalcitol  (Synonyms: KH1060)

Lexacalcitol (KH1060), a vitamin D analog, is a potent regulator of cell growth and immune responses. Lexacalcitol can be used for the research of graft rejection, psoriasis, cancer and auto-immune diseases^[1][2].

Lexacalcitol inhibits cell proliferation by 50% at 10^-12 M (14,000 times more active than la,25(OH)₂D₃) in human histiocytic lymphoma cell line U 937^[1].
Lexacalcitol inhibits interleukin-1-induced mouse thymocyte proliferation by 50% at 3×10^-16 M , allogeneic stimulation of mouse spleen lymphocytes at 5×10^-15 M^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Lexacalcitol (0.5 mg/kg/2 days; i.p.) in combination with cyclosporin A (CyA) can prevent autoimmune destruction of syngeneic islet grafts in spontaneously diabetic NOD recipients^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

460.69

C₂₉H₄₈O₄

131875-08-6

Solid

White to off-white

C[C@]1(CCC/2)[C@](CC[C@@H]1[C@@H](C)OCCCC(CC)(CC)O)([H])C2=C\C=C(C[C@@H](O)C[C@@H]3O)/C3=C

Room temperature in continental US; may vary elsewhere.

-20°C, protect from light, stored under nitrogen

*The compound is unstable in solutions, freshly prepared is recommended.

• [1]. L Binderup, et al. 20-epi-vitamin D3 analogues: a novel class of potent regulators of cell growth and immune responses. Biochem Pharmacol. 1991 Sep 27;42(8):1569-75.  [Content Brief]

  [2]. C Gysemans, et al. A combination of KH1060, a vitamin D(3) analogue, and cyclosporin prevents early graft failure and prolongs graft survival of xenogeneic islets in nonobese diabetic mice. Transplant Proc. 2001 May;33(3):2365.  [Content Brief]