U-73122
(Synonyms: 1-[6-[((17Β)-3-雌酮-1,3,5[10]-三烯-17-基)氨基]乙基]-1H-吡咯-2,5-二酮) 目录号 : GC10451
U-73122是有效的、选择性的磷脂酶C（PLC）抑制剂，IC50值约为1-2.1µM，也可抑制5-脂氧合酶（5-LO）。
Cas No.:112648-68-7
Sample solution is provided at 25 µL, 10mM.
U-73122 is a potent and selective phospholipase C (PLC) inhibitor with an IC50 value of approximately 1-2.1µM. It also inhibits 5-lipoxygenase (5-LO)[1]. U-73122 can inhibit Ca2+ release from the intracellular sarcoplasmic reticulum by inhibiting the Ca2+ pump[2]. U-73122 is a potent inhibitor of the smooth muscle endoplasmic reticulum calcium ATPase (SERCA) pump [3].
In vitro, treatment of human osteosarcoma MG-63 cells with U-73122 (1, 10µM) for 24h reduced cell number and cell-cell adhesion, significantly changed cell morphology, and rearranged the expression group of PLC enzymes [4]. Treatment of UMR-106 cells with U-73122 (0.2-10µM) for 3min dose-dependently inhibited calcium transients stimulated by endothelin-1 and parathyroid hormone[5]. U-73122 (2-12µM) treatment of β-TC3 cells dose-dependently inhibited the effects of carbachol on intracellular free calcium and insulin release[6].
In vivo, U-73122 (9mg/kg) treated wild-type mice by intraperitoneal injection for 15min significantly reduced cardiac TNF-α expression[7].
References:
[1] Sarabia-Sánchez M A, Moreno-Londoño A P, Castañeda-Patlán M C, et al. Non-canonical Wnt/Ca2+ signaling is essential to promote self-renewal and proliferation in colon cancer stem cells[J]. Frontiers in Oncology, 2023, 13: 1121787.
[2] Macmillan D, McCarron J G. The phospholipase C inhibitor U‐73122 inhibits Ca2+ release from the intracellular sarcoplasmic reticulum Ca2+ store by inhibiting Ca2+ pumps in smooth muscle[J]. British journal of pharmacology, 2010, 160(6): 1295-1301.
[3] Hollywood M A, Sergeant G P, Thornbury K D, et al. The PI‐PLC inhibitor U‐73122 is a potent inhibitor of the SERCA pump in smooth muscle[J]. British journal of pharmacology, 2010, 160(6): 1293-1294.
[4] Lo Vasco V R, Leopizzi M, Di Maio V, et al. U-73122 reduces the cell growth in cultured MG-63 ostesarcoma cell line involving Phosphoinositide-specific Phospholipases C[J]. Springerplus, 2016, 5(1): 156.
[5] Tatrai A, Suk K L, Stern P H. U-73122, a phospholipase C antagonist, inhibits effects of endothelin-1 and parathyroid hormone on signal transduction in UMR-106 osteoblastic cells[J]. Biochimica et Biophysica Acta (BBA)-Molecular Cell Research, 1994, 1224(3): 575-582.
[6] Chen T H, Hsu W H. U-73122 inhibits carbachol-induced increases in [Ca2+] i, IP3, and insulin release in β-TC3 cells[J]. Life sciences, 1994, 56(5): 103-108.
[7] Peng T, Shen E, Fan J, et al. Disruption of phospholipase Cγ1 signalling attenuates cardiac tumor necrosis factor-α expression and improves myocardial function during endotoxemia[J]. Cardiovascular research, 2008, 78(1): 90-97.
U-73122是有效的、选择性的磷脂酶C（PLC）抑制剂，IC50值约为1-2.1µM，也可抑制5-脂氧合酶（5-LO）[1]。U-73122可以通过抑制Ca2+泵来抑制细胞内肌浆网中的Ca2+释放[2]。U-73122是平滑肌肌内质网钙ATP酶（SERCA）泵的有效抑制剂[3]
在体外，U-73122（1、10µM）处理人骨肉瘤MG-63细胞24h，减少了细胞数量和细胞间粘附，细胞形态显著变化，PLC酶的表达组发生了重排[4]。U-73122（0.2-10µM）处理UMR-106细胞3min，剂量依赖性地抑制了内皮素-1和甲状旁腺激素刺激的钙瞬变[5]。U-73122（2-12µM）处理β-TC3细胞，剂量依赖性地抑制了卡巴胆碱对细胞内游离钙和胰岛素释放的影响[6]。
在体内，U-73122（9mg/kg）通过腹腔注射处理野生型小鼠15min，显著降低了心脏TNF-α表达[7]。
| Cell experiment [1]: | |
Cell lines | MG-63 cells |
Preparation Method | Cells were treated with DMSO, 1μM U-73122, and 10μM U-73122 for 24 hours. PCR analysis was performed on the cells at 0, 1, 3, 6, and 24h, and morphological experiments were performed at 18 and 24 hours. |
Reaction Conditions | 1、10µM; 24h |
Applications | U-73122 treatment reduced cell number and cell-cell adhesion, significantly altered cell morphology, and rearranged the expression profile of PLC enzymes. |
| Animal experiment [2]: | |
Animal models | Wild-type mice |
Preparation Method | Wild-type mice were treated with either U-73122 or its inactive analogue U-73343 (9mg/kg, i.p.) for 15 min, followed by LPS (4mg/kg, i.p.) for 4 h. |
Dosage form | 9mg/kg; i.p. |
Applications | U-73122 significantly attenuated TNF-a mRNA expression by 70%, compared with U-73343. |
References: [1]Lo Vasco V R, Leopizzi M, Di Maio V, et al. U-73122 reduces the cell growth in cultured MG-63 ostesarcoma cell line involving Phosphoinositide-specific Phospholipases C[J]. Springerplus, 2016, 5(1): 156. [2]Peng T, Shen E, Fan J, et al. Disruption of phospholipase Cγ1 signalling attenuates cardiac tumor necrosis factor-α expression and improves myocardial function during endotoxemia[J]. Cardiovascular research, 2008, 78(1): 90-97. | |
| Cas No. | 112648-68-7 | SDF | |
| 别名 | 1-[6-[((17Β)-3-雌酮-1,3,5[10]-三烯-17-基)氨基]乙基]-1H-吡咯-2,5-二酮 | ||
| 化学名 | 1-[6-[[(8R,9S,13S,14S,17S)-3-methoxy-13-methyl-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthren-17-yl]amino]hexyl]pyrrole-2,5-dione | ||
| Canonical SMILES | CC12CCC3C(C1CCC2NCCCCCCN4C(=O)C=CC4=O)CCC5=C3C=CC(=C5)OC | ||
| 分子式 | C29H40N2O3 | 分子量 | 464.64 |
| 溶解度 | ≥ 5.67mg/mL in DMSO with gentle warming, ≥ 15.5mg/mL in EtOH with ultrasonic and warming | 储存条件 | 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℃，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。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.1522 mL | 10.761 mL | 21.522 mL |
| 5 mM | 0.4304 mL | 2.1522 mL | 4.3044 mL |
| 10 mM | 0.2152 mL | 1.0761 mL | 2.1522 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet