LP-533401 hydrochloride
LP-533401 hydrochloride 是色an酸羥化酶 1 (tryptophan hydroxylase 1) 抑制劑，可以調(diào)節(jié)腸道中血清素的產(chǎn)生。
生物活性
LP-533401 hydrochloride is a tryptophan hydroxylase 1 inhibitor that regulates serotonin production in the gut.
IC50 & Target
Tryptophan hydroxylase 1[1]
體外研究(In Vitro)
LP-533401 hydrochloride is a tryptophan hydroxylase 1 inhibitor. LP-533401 (1 μM) completely inhibits serotonin production in Tph1-expressing cells (RBL2H3 cells) after treatment for 3 days[1].
體內(nèi)研究(In Vivo)
Oral administration once daily for up to 6 weeks of LP-533401 (25, 100 or 250 mg/kg) dose-dependently prevents the development of and fully rescues, osteoporosis in ovariectomized rodents because of an isolated increase in bone formation. Pharmacokinetic studies in rodents show that LP-533401 level in the brain is negligible following oral administration, indicating that it is virtually unable to cross the blood-brain barrier[1]. Mice treated repeatedly with LP-533401 (30-250 mg/kg per day) exhibit marked 5-HT content reductions in the gut, lungs, and blood, but not in the brain. After a single LP-533401 dose (250 mg/kg), lung and gut 5-HT contents decrease by 50%, whereas blood 5-HT levels remain unchanged, suggesting gut and lung 5-HT synthesis[2]. Adult, healthy mice treated with the Tph-1 inhibitor LP-533401 show 30% decrease in circulating serotonin levels, with a consequent 30% increase in osteoblast numbers. Administration of LP-533401 to mice injected with EL4 cells inhibits the decrement in osteoblast numbers and trabecular bone volume, prolongs survial, and decreases leukemic infiltration[3].
分子量：562.94
性狀：Solid
Formula：C27H23ClF4N4O3
CAS 號(hào)：1040526-12-2
運(yùn)輸條件：Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式
4°C, sealed storage, away from moisture
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶解性數(shù)據(jù)
DMSO : 25 mg/mL (44.41 mM; Need ultrasonic)
H2O : < 0.1 mg/mL (insoluble)
| 濃度溶劑體積質(zhì)量 | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.7764 mL | 8.8819 mL | 17.7639 mL |
| 5 mM | 0.3553 mL | 1.7764 mL | 3.5528 mL |
| 10 mM | 0.1776 mL | 0.8882 mL | 1.7764 mL |
請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 儲(chǔ)存時(shí)，請?jiān)?6 個(gè)月內(nèi)使用，-20°C 儲(chǔ)存時(shí)，請?jiān)?1 個(gè)月內(nèi)使用。
以下溶解方案都請先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用； 以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶
- 1.
請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (4.44 mM); Clear solution
- 2.
請依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: 2.5 mg/mL (4.44 mM); Suspended solution; Need ultrasonic
參考文獻(xiàn)
[1]. Yadav, V.K., et al. Inhibition of gut-derived serotonin synthesis: A potential bone anabolic treatment. Nat. Med. 16(3), 308-312 (2010).
[2]. Abid S, et al. Inhibition of gut- and lung-derived serotonin attenuates pulmonary hypertension in mice. Am J Physiol Lung Cell Mol Physiol. 2012 Sep 15;303(6):L500-8. [Content Brief]
[3]. Krevvata M, et al. Inhibition of leukemia cell engraftment and disease progression in mice by osteoblasts. Blood. 2014 Oct 30;124(18):2834-46. [Content Brief]
注：產(chǎn)品僅用于科研
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