GlpBio

Pregnenolone sulfate (sodium salt)

目录号: GC44680纯度: >98.00%同义词: 3β-Hydroxy-5-pregnen-20-one monosulfate sodium
Pregnenolone sulfate (sodium salt)是一种孕烯醇酮的神经活性代谢产物，对氨基丁酸A型受体（GABAAR）的IC50值为26±2μmol/L，对不含γ亚基的GABAAR的IC50值为18±3μmol/L。
Pregnenolone sulfate (sodium salt)
Cas No.: 1852-38-6
规格价格库存数量操作
50mg¥700.00现货
1
100mg¥1,120.00现货
1
250mg¥2,282.00现货
1
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产品描述 Description

Pregnenolone sulfate (sodium salt), a neuroactive metabolite of pregnenolone, exhibits the IC50 value of 26±2μmol/L for the aminobutyric acid type A receptor (GABAAR) and the IC50 value of 18±3μmol/L for GABAAR without the γ subunit[1]. Pregnenolone sulfate is a potent enhancer of intracellular Ca2+, with the EC50 value of 2pmol/L[2]. Pregnenolone sulfate has been used in neurological studies and seizure studies[3].

In vitro, Pregnenolone sulfate (200μmol/L) treatment for 24 hours significantly inhibited human T cell proliferation and viability[4]. Pregnenolone sulfate suppressed acetylcholine-induced catecholamine secretion (IC50=27μmol/L) and inhibited the Ca2+(IC50=20μmol/L) influx in bovine adrenal chromaffin cells after 10min treatment[5]. Pregnenolone sulfate (100μmol/L, 10 seconds) promoted NR1 movement to the cell surface in Xenopus laevis oocytes expressing NR1/NR2A a G protein-coupled pathway that requires both intracellular Ca2+ and phospholipase C activation[6].

In vivo, Pregnenolone sulfate (10mg/kg/day, s.c.) treatment for 4 days in adult male rats resulted in cognitive enhancement, with improvement in spatial orientation acquisition[7]. Subcutaneous injection of Pregnenolone sulfate (40mg/kg) for 30 minutes significantly shortened the immobility time and promoted the movement of male albino mice[8].

References:
[1] Sachidanandan D, Bera A K. Inhibition of the GABA A receptor by sulfated neurosteroids: a mechanistic comparison study between pregnenolone sulfate and dehydroepiandrosterone sulfate[J]. Journal of Molecular Neuroscience, 2015, 56: 868-877.
[2] Smith C C, Martin S C, Sugunan K, et al. A role for picomolar concentrations of pregnenolone sulfate in synaptic activity-dependent Ca2+ signaling and CREB activation[J]. Molecular pharmacology, 2014, 86(4): 390-398.
[3] Williamson J, Mtchedlishvili Z, Kapur J. Characterization of the convulsant action of pregnenolone sulfate[J]. Neuropharmacology, 2004, 46(6): 856-864.
[4] El Hajj Y, Shahin T, Dieng M M, et al. Pregnenolone sulfate induces transcriptional and immunoregulatory effects on T cells[J]. Scientific reports, 2024, 14(1): 6782.
[5] Kudo K, Tachikawa E, Kashimoto T. Inhibition by pregnenolone sulfate of nicotinic acetylcholine response in adrenal chromaffin cells[J]. European journal of pharmacology, 2002, 456(1-3): 19-27.
[6] Kostakis E, Smith C, Jang M K, et al. The neuroactive steroid pregnenolone sulfate stimulates trafficking of functional N-methyl D-aspartate receptors to the cell surface via a noncanonical, G protein, and Ca2+-dependent mechanism[J]. Molecular pharmacology, 2013, 84(2): 261-274.
[7] Plescia F, Sardo P, Rizzo V, et al. Pregnenolone sulphate enhances spatial orientation and object discrimination in adult male rats: evidence from a behavioural and electrophysiological study[J]. Behavioural brain research, 2014, 258: 193-201.
[8] Dhir A, Kulkarni S K. Involvement of sigma (σ1) receptors in modulating the anti-depressant effect of neurosteroids (dehydroepiandrosterone or pregnenolone) in mouse tail-suspension test[J]. Journal of Psychopharmacology, 2008, 22(6): 691-696.

Pregnenolone sulfate (sodium salt)是一种孕烯醇酮的神经活性代谢产物，对氨基丁酸A型受体（GABAAR）的IC50值为26±2μmol/L，对不含γ亚基的GABAAR的IC50值为18±3μmol/L[1]。Pregnenolone sulfate能显著增强细胞内钙离子浓度，EC50值为2pmol/L[2]。Pregnenolone sulfate已被应用于神经学研究和癫痫发作研究领域[3]。

在体外，Pregnenolone sulfate（200μmol/L）处理24小时能显著抑制人类T细胞增殖和细胞活性[4]。Pregnenolone sulfate处理牛肾上腺嗜铬细胞10分钟后可抑制乙酰胆碱诱导的儿茶酚胺分泌（IC50=27μmol/L），并阻断Ca2+内流（IC50=20μmol/L）[5]。在表达NR1/NR2A的非洲爪蟾卵母细胞中，Pregnenolone sulfate（100μmol/L，10秒）通过依赖细胞内Ca2+和磷脂酶C激活的G蛋白偶联通路，促进NR1亚基向细胞膜表面转运[6]。

在体内，Pregnenolone sulfate（10mg/kg/day，皮下注射）连续给药4天可显著增强成年雄性大鼠的认知功能，并改善大鼠的空间定向学习能力[7]。皮下注射Pregnenolone sulfate（40mg/kg）30分钟后能显著缩短雄性白化小鼠的静止不动时间，并促进运动行为[8]。

实验参考方法 Experimental Reference Method

Cell experiment [1]:

Cell lines

Bovine adrenal chromaffin cells

Preparation Method

Bovine adrenal chromaffin cells were mixed with Eagle's minimum essential medium and 10% calf serum and then added with antibiotics (100units/ml of penicillin, 100μg/ml of streptomycin and 0.3μg/ml of amphotericin B) plus 3μmol/L cytosine arabinoside before seeding cells on 35-mm diameter plastic culture dishes at 2×106cells per dish for monolayer culture. The cells needed for [3H]nicotine binding analysis were plated onto 24-well plates at 5×105cells per well. For four days the cells were kept at 37°C in a humidified incubator with 95% air and 5% CO2 atmosphere. 2×106cells contained 34.6±4.2μg of epinephrine and norepinephrine catecholamines combined. Following a 10-minute preincubation at 37°C in Krebs–Ringer–HEPES buffer (KRH buffer) with or without Pregnenolone sulfate (3-100μmol/L), the cells received further incubation in KRH buffer containing Ca2+ (37kBq) with or without Pregnenolone sulfate alongside either 50μmol/L acetylcholine or 56mmol/L K+ for 7 minutes. Following incubation medium removal, rapidly cool cells on ice before performing three washes with ice-cold KRH buffer lacking calcium but containing 10mmol/L LaCl3 and 2mmol/L EGTA. 10% Triton X-100 was added to the cells, which were then physically scraped off. The scintillation vials received the lysate mixed with scintillation fluid. The liquid scintillation counter measured the radioactivity levels.

Reaction Conditions

3-100μmol/L; 10min

Applications

Pregnenolone sulfate (3-100μmol/L) significantly inhibited acetylcholine-induced Ca2+ influx in a concentration-dependent manner within bovine adrenal chromaffin cells.
Animal experiment [2]:

Animal models

Male Wistar rats

Preparation Method

Adult male Wistar rats were used as subjects for experimental procedures. Standard plastic cages held two animals each inside a room with controlled temperature at 22±2°C and humidity at 55±10%. The colony followed a 12-hour light-dark cycle from 8:00 to 20:00 while food and water remained accessible at all times. On the behavioral testing day, administer subcutaneously Pregnenolone sulfate at 10mg/kg to 16 rats, whilst another group of 16 rats received injections of vehicle consisting of 0.1% Tween 80. Pregnenolone sulfate dissolved in 0.1% Tween 80 was administered subcutaneously at a dose of 1ml/kg two hours before each experimental session to monitor minor inter-individual variability in effects. The control group received identical volume of vehicle at the same time. The rats entered the laboratory on test days and had at least a 60-minute acclimatization period before beginning experimental sessions. All experimental sessions took place in sound-isolated chambers from 8:00 to 14:00. A television camera in an adjacent room captured the animal's performance. All devices received a thorough cleaning before each animal introduction to eliminate any effects on behavior from the detection of another rat's scent by the test subject.

Dosage form

10mg/kg/day; s.c.

Applications

Pregnenolone sulfate treatment in rats can exert cognitive enhancement, improving spatial orientation acquisition and object discrimination.

References:
[1] Kudo K, Tachikawa E, Kashimoto T. Inhibition by pregnenolone sulfate of nicotinic acetylcholine response in adrenal chromaffin cells[J]. European journal of pharmacology, 2002, 456(1-3): 19-27.
[2] Plescia F, Sardo P, Rizzo V, et al. Pregnenolone sulphate enhances spatial orientation and object discrimination in adult male rats: evidence from a behavioural and electrophysiological study[J]. Behavioural brain research, 2014, 258: 193-201.

产品文档 Product Documents

Purity:>98.00%

化学性质Chemical Properties

CAS 号
1852-38-6
同义词
3β-Hydroxy-5-pregnen-20-one monosulfate sodium
SMILES
C[C@]12C(C[C@@H](OS([O-])(=O)=O)CC2)=CC[C@]3([H])[C@]1([H])CC[C@@]4(C)[C@@]3([H])CC[C@@H]4C(C)=O.[Na+]
分子式
C21H31O5S•Na
分子量
418.5 g/mol
溶解性
30 mg/ml in DMSO(Need ultrasonic); 2 mg/ml in Ethanol.
保存条件
Store at -20°C
General tips
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；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

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