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Rosiglitazone (羅格列酮; BRL 49653)

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Rosiglitazone (BRL 49653)，是噻唑烷二酮類胰島素增敏劑，也是選擇性的，具有口服活性 PPARγ 激動劑，對 PPARγ1、PPARγ2 和 PPARγ 的 EC50 值分別為 30 nM、100 nM 和 60 nM。Rosiglitazone 與 PPARγ 結(jié)合，Kd 約為 40 nM。Rosiglitazone 也是 TRPC5 的ji活劑 (EC50=～30 μM) 和 TRPM3 的抑制劑。

貨號：HY-17386
CAS：122320-73-4
參數(shù)品牌：MCE
產(chǎn)品參數(shù)
品牌：MCE
型號：HY-17386
起訂量：1
規(guī)格:：50mg
價格:：￥600
我知道了
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產(chǎn)品詳情

Rosiglitazone (Synonyms: 羅格列酮; BRL 49653)


Rosiglitazone (BRL 49653)，是噻唑烷二酮類胰島素增敏劑，也是選擇性的，具有口服活性 PPARγ 激動劑，對 PPARγ1、PPARγ2 和 PPARγ 的 EC50 值分別為 30 nM、100 nM 和 60 nM。Rosiglitazone 與 PPARγ 結(jié)合，Kd 約為 40 nM。Rosiglitazone 也是 TRPC5 的ji活劑 (EC50=～30 μM) 和 TRPM3 的抑制劑。

生物活性

Rosiglitazone (BRL 49653) is a selective, orally active PPARγ agonist with EC50s of 30 nM, 100 nM and 60 nM for PPARγ1, PPARγ2, and PPARγ, respectively. Rosiglitazone binds to PPARγ with a Kd of approximately 40 nM. Rosiglitazone is also an activator of TRPC5 (EC50=~30 μM) and an inhibitor of TRPM3[1][2][3][4].


體外研究(In Vitro)

Rosiglitazone is a potent and selective activator of PPARγ, with EC50s of 30 nM and 100 nM for PPARγ1 and PPARγ2, respectively, and a Kd of appr 40 nM for PPARγ. Rosiglitazone (BRL49653, 0.1, 1,10 μM) promotes differentiation of C3H10T1/2 stem cells to adipocytes[1]. Rosiglitazone (Compound 6) activates PPARγ, with an EC50 of 60 nM[2]. Rosiglitazone (1 μM) activates PPARγ, which binds to NF-α1 promoter to activate gene transcription in neurons. Rosiglitazone (1 μM) also protects Neuro2A cells and hippocampal neurons against oxidative stress, and up-regulates BCL-2 expression in an NF-α1-dependent manner[3]. Rosiglitazone completely inhibits TRPM3 with IC50 values of 9.5 and 4.6 μM against nifedipine- and PregS-evoked activity, but such effects are not via PPARγ. Rosiglitazone inhibits TRPM2 at higher concentration, with an IC50 of appr 22.5 μM. Rosiglitazone is a strong stimulator of TRPC5 channels, with an EC50 of ~30 μM[4].


體內(nèi)研究(In Vivo)

Rosiglitazone (5 mg/kg, p.o.) decreases the serum glucose in diabetic rats. Rosiglitazone also decreases IL-6, TNF-α, and VCAM-1 levels in diabetic group. Rosiglitazone in combination with losartan increases glucose compared to diabetic and Los-treated groups. Rosiglitazone significantly ameliorates endothelial dysfunction indicated by a significantly lower contractile response to PE and Ang II and enhancement of ACh-provoked relaxation in aortas isolated from diabetic rats[5].


分子量：357.43


Formula：C18H19N3O3S


CAS 號：122320-73-4


中文名稱：羅格列酮


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)

In Vitro: 

DMSO : 250 mg/mL (699.44 mM; Need ultrasonic)

Ethanol : 2 mg/mL (5.60 mM; ultrasonic and warming and heat to 60°C)

H2O : < 0.1 mg/mL (ultrasonic) (insoluble)

配制儲備液
濃度溶劑體積質(zhì)量1 mg5 mg10 mg
1 mM2.7978 mL13.9888 mL27.9775 mL
5 mM0.5596 mL2.7978 mL5.5955 mL
10 mM0.2798 mL1.3989 mL2.7978 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： 5% DMSO    40% PEG300    5% Tween-80    50% saline

    Solubility: ≥ 2.5 mg/mL (6.99 mM); Clear solution


  • 2.


    請依序添加每種溶劑： 5% DMSO    95% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.99 mM); Clear solution


  • 3.


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

    Solubility: ≥ 2.08 mg/mL (5.82 mM); Clear solution


  • 4.


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

    Solubility: ≥ 2.08 mg/mL (5.82 mM); Clear solution


  • 5.


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

    Solubility: ≥ 2.08 mg/mL (5.82 mM); Clear solution

參考文獻

[1]. Lehmann JM, et al. An antidiabetic thiazolidinedione is a high affinity ligand for peroxisome proliferator-activated receptor gamma (PPAR gamma). J Biol Chem. 1995 Jun 2;270(22):12953-6.

[2]. Willson TM, et al. The structure-activity relationship between peroxisome proliferator-activated receptor gamma agonism and the antihyperglycemic activity of thiazolidinediones. J Med Chem. 1996 Feb 2;39(3):665-8.

[3]. Thouennon E, et al. Rosiglitazone-activated PPARγ induces neurotrophic factor-α1 transcription contributing to neuroprotection. J Neurochem. 2015 Aug;134(3):463-70.

[4]. Majeed Y, et al. Rapid and contrasting effects of rosiglitazone on transient receptor potential TRPM3 and TRPC5 channels. Mol Pharmacol. 2011 Jun;79(6):1023-30.

[5]. Ateyya H, et al. Beneficial effects of rosiglitazone and losartan combination in diabetic rats. Can J Physiol Pharmacol. 2018 Mar;96(3):215-220.


Rosiglitazone (羅格列酮; BRL 49653)

Rosiglitazone (羅格列酮; BRL 49653)

分享到微信

×
Rosiglitazone (BRL 49653)，是噻唑烷二酮類胰島素增敏劑，也是選擇性的，具有口服活性 PPARγ 激動劑，對 PPARγ1、PPARγ2 和 PPARγ 的 EC50 值分別為 30 nM、100 nM 和 60 nM。Rosiglitazone 與 PPARγ 結(jié)合，Kd 約為 40 nM。Rosiglitazone 也是 TRPC5 的ji活劑 (EC50=～30 μM) 和 TRPM3 的抑制劑。

貨號：HY-17386
CAS：122320-73-4
品牌：MCE
型號：HY-17386
起訂量：1
規(guī)格:：50mg
價格:：￥600
15906629305
在線客服
產(chǎn)品詳情

Rosiglitazone (Synonyms: 羅格列酮; BRL 49653)


Rosiglitazone (BRL 49653)，是噻唑烷二酮類胰島素增敏劑，也是選擇性的，具有口服活性 PPARγ 激動劑，對 PPARγ1、PPARγ2 和 PPARγ 的 EC50 值分別為 30 nM、100 nM 和 60 nM。Rosiglitazone 與 PPARγ 結(jié)合，Kd 約為 40 nM。Rosiglitazone 也是 TRPC5 的ji活劑 (EC50=～30 μM) 和 TRPM3 的抑制劑。

生物活性

Rosiglitazone (BRL 49653) is a selective, orally active PPARγ agonist with EC50s of 30 nM, 100 nM and 60 nM for PPARγ1, PPARγ2, and PPARγ, respectively. Rosiglitazone binds to PPARγ with a Kd of approximately 40 nM. Rosiglitazone is also an activator of TRPC5 (EC50=~30 μM) and an inhibitor of TRPM3[1][2][3][4].


體外研究(In Vitro)

Rosiglitazone is a potent and selective activator of PPARγ, with EC50s of 30 nM and 100 nM for PPARγ1 and PPARγ2, respectively, and a Kd of appr 40 nM for PPARγ. Rosiglitazone (BRL49653, 0.1, 1,10 μM) promotes differentiation of C3H10T1/2 stem cells to adipocytes[1]. Rosiglitazone (Compound 6) activates PPARγ, with an EC50 of 60 nM[2]. Rosiglitazone (1 μM) activates PPARγ, which binds to NF-α1 promoter to activate gene transcription in neurons. Rosiglitazone (1 μM) also protects Neuro2A cells and hippocampal neurons against oxidative stress, and up-regulates BCL-2 expression in an NF-α1-dependent manner[3]. Rosiglitazone completely inhibits TRPM3 with IC50 values of 9.5 and 4.6 μM against nifedipine- and PregS-evoked activity, but such effects are not via PPARγ. Rosiglitazone inhibits TRPM2 at higher concentration, with an IC50 of appr 22.5 μM. Rosiglitazone is a strong stimulator of TRPC5 channels, with an EC50 of ~30 μM[4].


體內(nèi)研究(In Vivo)

Rosiglitazone (5 mg/kg, p.o.) decreases the serum glucose in diabetic rats. Rosiglitazone also decreases IL-6, TNF-α, and VCAM-1 levels in diabetic group. Rosiglitazone in combination with losartan increases glucose compared to diabetic and Los-treated groups. Rosiglitazone significantly ameliorates endothelial dysfunction indicated by a significantly lower contractile response to PE and Ang II and enhancement of ACh-provoked relaxation in aortas isolated from diabetic rats[5].


分子量：357.43


Formula：C18H19N3O3S


CAS 號：122320-73-4


中文名稱：羅格列酮


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)

In Vitro: 

DMSO : 250 mg/mL (699.44 mM; Need ultrasonic)

Ethanol : 2 mg/mL (5.60 mM; ultrasonic and warming and heat to 60°C)

H2O : < 0.1 mg/mL (ultrasonic) (insoluble)

配制儲備液
濃度溶劑體積質(zhì)量1 mg5 mg10 mg
1 mM2.7978 mL13.9888 mL27.9775 mL
5 mM0.5596 mL2.7978 mL5.5955 mL
10 mM0.2798 mL1.3989 mL2.7978 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： 5% DMSO    40% PEG300    5% Tween-80    50% saline

    Solubility: ≥ 2.5 mg/mL (6.99 mM); Clear solution


  • 2.


    請依序添加每種溶劑： 5% DMSO    95% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.99 mM); Clear solution


  • 3.


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

    Solubility: ≥ 2.08 mg/mL (5.82 mM); Clear solution


  • 4.


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

    Solubility: ≥ 2.08 mg/mL (5.82 mM); Clear solution


  • 5.


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

    Solubility: ≥ 2.08 mg/mL (5.82 mM); Clear solution

參考文獻

[1]. Lehmann JM, et al. An antidiabetic thiazolidinedione is a high affinity ligand for peroxisome proliferator-activated receptor gamma (PPAR gamma). J Biol Chem. 1995 Jun 2;270(22):12953-6.

[2]. Willson TM, et al. The structure-activity relationship between peroxisome proliferator-activated receptor gamma agonism and the antihyperglycemic activity of thiazolidinediones. J Med Chem. 1996 Feb 2;39(3):665-8.

[3]. Thouennon E, et al. Rosiglitazone-activated PPARγ induces neurotrophic factor-α1 transcription contributing to neuroprotection. J Neurochem. 2015 Aug;134(3):463-70.

[4]. Majeed Y, et al. Rapid and contrasting effects of rosiglitazone on transient receptor potential TRPM3 and TRPC5 channels. Mol Pharmacol. 2011 Jun;79(6):1023-30.

[5]. Ateyya H, et al. Beneficial effects of rosiglitazone and losartan combination in diabetic rats. Can J Physiol Pharmacol. 2018 Mar;96(3):215-220.


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