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IBMX

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IBMX 是一種廣譜的磷酸二酯酶 (PDE) 抑制劑，抑制 PDE3，PDE4 和 PDE5，IC50 分別為 6.5，26.3 和 31.7 μM。貨號：HY-12318，CAS:28822-58-4
參數(shù)品牌：MCE
產(chǎn)品參數(shù)
品牌：MCE
型號：HY-12318
起訂量：1
規(guī)格:：50mg
價格:：￥500
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產(chǎn)品詳情

IBMX (Synonyms: 3-Isobutyl-1-methylxanthine; Isobutylmethylxanthine)

IBMX 是一種廣譜的磷酸二酯酶 (PDE) 抑制劑，抑制 PDE3，PDE4 和 PDE5，IC50 分別為 6.5，26.3 和 31.7 μM。

生物活性

IBMX is a broad-spectrum phosphodiesterase (PDE) inhibitor, with IC50s of 6.5, 26.3 and 31.7 μM for PDE3, PDE4 and PDE5, respectively.


IC50 & Target：IC50: 6.5±1.2 μM(PDE3), 26.3±3.9 μM (PDE4), 31.7±5.3 μM (PDE5)[1]


體外研究(In Vitro)

At 100 μM, KMUP-1 (a xanthine derivative) and IBMX are the most effective at inducing tracheal relaxation; the magnitude of the relaxation responses induced by KMUP-1 and IBMX are not significantly different[1]. IBMX (100 μM) activates renal outer medullary K+ (ROMK) channels (n=6, P<0.05) and prevents further channel activation by ANG II (n=6, P=NS) or cGMP. Of note is that pretreatment of cortical collecting duct (CCDs) isolated from high-K+ (HK)-fed rats with IBMX (100 μM) for 20 min leads to a significant increase in tubular cAMP content to 1.43±0.35 pg/mm tubule length (n=14) compare with that measured in vehicle-treated controls (0.61±0.13 pg/mm tubule length, n=12, P<0.05)


體內(nèi)研究(In Vivo)

IBMX, a non-selective PDE inhibitor significantly decreases the liver glycogen storage (mg/g, IBMX 22±1.5 P<0.001). In comparison with the control group, IBMX and mc5 significantly increase plasma glucose (blood glucose, mg/dl, control=141±3, IBMX=210±17 P<0.001 and mc5=191±13 P<0.01) while other test compounds (mc1, mc6, MCPIP and Win 47203) do not produce significant effect (control=141±3, mc1 160±7, mc6 175±9, MCPIP 179±8 and Win 47203 116±2 P>0.05) also mc2 does not change plasma glucose (control=141±3 and mc2=145±5). IBMX has the highest efficacy on increasing plasma glucose[3]. Treatments with IBMX and Apocynin significantly decrease cold-induced elevation of right ventricular (RV) systolic pressure (23.5±1.8 and 24.2±0.6 mmHg, respectively) although they do not decrease RV pressure to the warm control levels. IBMX or Apocynin significantly reduces medial layer thickness (19.0±0.9, and 16.9±0.8 μm, respectively) and increases lumen diameter (62.7±4.2, and 59.5±4.3 μm, respectively) of small PAs in cold-exposed rats


分子量：222.24


Formula：C10H14N4O2


CAS 號：28822-58-4


運輸條件：Room temperature in continental US; may vary elsewhere.


儲存方式

Powder-20°C3 years

4°C2 years
In solvent-80°C6 months

-20°C1 month


溶解性數(shù)據(jù)


DMSO : 50 mg/mL (224.98 mM; Need ultrasonic)

Ethanol : ≥ 7.14 mg/mL (32.13 mM)

* "≥" means soluble, but saturation unknown.

配制儲備液
濃度溶劑體積質(zhì)量1 mg5 mg10 mg
1 mM4.4996 mL22.4982 mL44.9964 mL
5 mM0.8999 mL4.4996 mL8.9993 mL
10 mM0.4500 mL2.2498 mL4.4996 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。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 儲存時，請在 6 個月內(nèi)使用，-20°C 儲存時，請在 1 個月內(nèi)使用。

In Vivo:

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：

——為保證實驗結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的工作液，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: ≥ 1.67 mg/mL (7.51 mM); Clear solution


  • 2.


    請依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 1.67 mg/mL (7.51 mM); Suspended solution; Need ultrasonic


  • 3.


    請依序添加每種溶劑： 10% DMSO    90% corn oil

    Solubility: ≥ 1.67 mg/mL (7.51 mM); Clear solution


  • 4.


    請依序添加每種溶劑： 10% EtOH    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 0.71 mg/mL (3.19 mM); Clear solution


  • 5.


    請依序添加每種溶劑： 10% EtOH    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 0.71 mg/mL (3.19 mM); Clear solution


  • 6.


    請依序添加每種溶劑： 10% EtOH    90% corn oil

    Solubility: ≥ 0.71 mg/mL (3.19 mM); Clear solution


參考文獻

[1]. Wu BN, et al. KMUP-1, a xanthine derivative, induces relaxation of guinea-pig isolated trachea: the role of the epithelium, cyclic nucleotides and K+ channels. Br J Pharmacol. 2004 Aug;142(7):1105-14

[2]. Wei Y, et al. Angiotensin II type 2 receptor regulates ROMK-like K+ channel activity in the renal cortical collecting duct during high dietary K+ adaptation. Am J Physiol Renal Physiol. 2014 Oct 1;307(7):F833-43

[3]. Hosseini A, et al. Differential metabolic effects of novel cilostamide analogs, methyl carbostiryl derivatives, on mouse and hyperglycemic rat. Iran J Basic Med Sci. 2012 Jul;15(4):916-25.

[4]. Crosswhite P, et al. Inhibition of phosphodiesterase-1 attenuates cold-induced pulmonary hypertension. Hypertension. 2013 Mar;61(3):585-92.


IBMX

IBMX

分享到微信

×
IBMX 是一種廣譜的磷酸二酯酶 (PDE) 抑制劑，抑制 PDE3，PDE4 和 PDE5，IC50 分別為 6.5，26.3 和 31.7 μM。貨號：HY-12318，CAS:28822-58-4
品牌：MCE
型號：HY-12318
起訂量：1
規(guī)格:：50mg
價格:：￥500
15906629305
在線客服
產(chǎn)品詳情

IBMX (Synonyms: 3-Isobutyl-1-methylxanthine; Isobutylmethylxanthine)

IBMX 是一種廣譜的磷酸二酯酶 (PDE) 抑制劑，抑制 PDE3，PDE4 和 PDE5，IC50 分別為 6.5，26.3 和 31.7 μM。

生物活性

IBMX is a broad-spectrum phosphodiesterase (PDE) inhibitor, with IC50s of 6.5, 26.3 and 31.7 μM for PDE3, PDE4 and PDE5, respectively.


IC50 & Target：IC50: 6.5±1.2 μM(PDE3), 26.3±3.9 μM (PDE4), 31.7±5.3 μM (PDE5)[1]


體外研究(In Vitro)

At 100 μM, KMUP-1 (a xanthine derivative) and IBMX are the most effective at inducing tracheal relaxation; the magnitude of the relaxation responses induced by KMUP-1 and IBMX are not significantly different[1]. IBMX (100 μM) activates renal outer medullary K+ (ROMK) channels (n=6, P<0.05) and prevents further channel activation by ANG II (n=6, P=NS) or cGMP. Of note is that pretreatment of cortical collecting duct (CCDs) isolated from high-K+ (HK)-fed rats with IBMX (100 μM) for 20 min leads to a significant increase in tubular cAMP content to 1.43±0.35 pg/mm tubule length (n=14) compare with that measured in vehicle-treated controls (0.61±0.13 pg/mm tubule length, n=12, P<0.05)


體內(nèi)研究(In Vivo)

IBMX, a non-selective PDE inhibitor significantly decreases the liver glycogen storage (mg/g, IBMX 22±1.5 P<0.001). In comparison with the control group, IBMX and mc5 significantly increase plasma glucose (blood glucose, mg/dl, control=141±3, IBMX=210±17 P<0.001 and mc5=191±13 P<0.01) while other test compounds (mc1, mc6, MCPIP and Win 47203) do not produce significant effect (control=141±3, mc1 160±7, mc6 175±9, MCPIP 179±8 and Win 47203 116±2 P>0.05) also mc2 does not change plasma glucose (control=141±3 and mc2=145±5). IBMX has the highest efficacy on increasing plasma glucose[3]. Treatments with IBMX and Apocynin significantly decrease cold-induced elevation of right ventricular (RV) systolic pressure (23.5±1.8 and 24.2±0.6 mmHg, respectively) although they do not decrease RV pressure to the warm control levels. IBMX or Apocynin significantly reduces medial layer thickness (19.0±0.9, and 16.9±0.8 μm, respectively) and increases lumen diameter (62.7±4.2, and 59.5±4.3 μm, respectively) of small PAs in cold-exposed rats


分子量：222.24


Formula：C10H14N4O2


CAS 號：28822-58-4


運輸條件：Room temperature in continental US; may vary elsewhere.


儲存方式

Powder-20°C3 years

4°C2 years
In solvent-80°C6 months

-20°C1 month


溶解性數(shù)據(jù)


DMSO : 50 mg/mL (224.98 mM; Need ultrasonic)

Ethanol : ≥ 7.14 mg/mL (32.13 mM)

* "≥" means soluble, but saturation unknown.

配制儲備液
濃度溶劑體積質(zhì)量1 mg5 mg10 mg
1 mM4.4996 mL22.4982 mL44.9964 mL
5 mM0.8999 mL4.4996 mL8.9993 mL
10 mM0.4500 mL2.2498 mL4.4996 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。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 儲存時，請在 6 個月內(nèi)使用，-20°C 儲存時，請在 1 個月內(nèi)使用。

In Vivo:

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：

——為保證實驗結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的工作液，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: ≥ 1.67 mg/mL (7.51 mM); Clear solution


  • 2.


    請依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 1.67 mg/mL (7.51 mM); Suspended solution; Need ultrasonic


  • 3.


    請依序添加每種溶劑： 10% DMSO    90% corn oil

    Solubility: ≥ 1.67 mg/mL (7.51 mM); Clear solution


  • 4.


    請依序添加每種溶劑： 10% EtOH    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 0.71 mg/mL (3.19 mM); Clear solution


  • 5.


    請依序添加每種溶劑： 10% EtOH    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 0.71 mg/mL (3.19 mM); Clear solution


  • 6.


    請依序添加每種溶劑： 10% EtOH    90% corn oil

    Solubility: ≥ 0.71 mg/mL (3.19 mM); Clear solution


參考文獻

[1]. Wu BN, et al. KMUP-1, a xanthine derivative, induces relaxation of guinea-pig isolated trachea: the role of the epithelium, cyclic nucleotides and K+ channels. Br J Pharmacol. 2004 Aug;142(7):1105-14

[2]. Wei Y, et al. Angiotensin II type 2 receptor regulates ROMK-like K+ channel activity in the renal cortical collecting duct during high dietary K+ adaptation. Am J Physiol Renal Physiol. 2014 Oct 1;307(7):F833-43

[3]. Hosseini A, et al. Differential metabolic effects of novel cilostamide analogs, methyl carbostiryl derivatives, on mouse and hyperglycemic rat. Iran J Basic Med Sci. 2012 Jul;15(4):916-25.

[4]. Crosswhite P, et al. Inhibition of phosphodiesterase-1 attenuates cold-induced pulmonary hypertension. Hypertension. 2013 Mar;61(3):585-92.


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