Vitamin D3 (Cholecalciferol; Colecalciferol) is a naturally occuring form of vitamin D. Vitamin D3 induces cell differentiation and prevents proliferation of cancer cells.

Vitamin D3 is an inactive vitamin D molecule in vivo. Vitamin D3 undergoes two hydroxylation processes to activate it. Vitamin D3 is first hydroxylated in the liver to form the circulating prohormone 25-hydroxy vitamin D3 [25(OH)D3] by the enzyme 25-hydroxylase (CYP27A1) and probably also by other enzymes (e.g., CYP2R1)^[1].
The second hydroxylation occurs in the kidneys via the enzyme 1-alpha-hydroxylase, yielding 1,25- dihydroxycholecalciferol (calcitriol), which is the biologically active form of vitamin D^[1].
Vitamin D3 (2-10 μM; 24-48 hours) exhibits anti-proliferative effects in a dose- and time- dependent manner. Maximal reduction of viability post treatment of 62% (IK), 52% (RL-95-2), and 55% (Hec-1A) occurrs by 72 h of treatment with 10 μM Vitamin D3. but 24-hour exposure lacks significant reduction in viable cells^[2].
Cholecalciferol (10 μM; 24-48 hours) shows marked increases in nuclear VDR staining and produces local VDR activation in IK cells^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cholecalciferol (oral gavage; 5 mg/kg; 7 days) potentiates the CCl4 toxicity only in the liver, as indicated by plasma levels of ALT and AST, biochemical markers of hepatic damage. It significantly increases renal calcium levels in mice, but renal calcium content does not differ significantly between mice^[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

384.64

C₂₇H₄₄O

67-97-0

维生素D3；胆骨化醇

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请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液；该产品在溶液状态不稳定，建议您现用现配，即刻使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

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• 1.

  请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

  Solubility: ≥ 2.08 mg/mL (5.41 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (5.41 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

• 2.

  请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

  Solubility: 2.08 mg/mL (5.41 mM); Suspended solution; Need ultrasonic

  此方案可获得 2.08 mg/mL (5.41 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

  以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

  将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
• 3.

  请依序添加每种溶剂： 10% DMSO    90% corn oil

  Solubility: ≥ 2.08 mg/mL (5.41 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (5.41 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• [1]. Nazik Al-Hashimi, et al. Cholecalciferol

  [2]. Laura Bergadà, et al. Role of local bioactivation of vitamin D by CYP27A1 and CYP2R1 in the control of cell growth in normal endometrium and endometrial carcinoma. Lab Invest. 2014 Jun;94(6):608-22

  [3]. Hiroki Yoshioka, et al. Vitamin D3-induced hypercalcemia increases carbon tetrachloride-induced hepatotoxicity through elevated oxidative stress in mice. PLoS One. 2017 Apr 27;12(4):e0176524.