L-796568 free base
L-796568 free base is a β(3)-adrenergic receptor agonist. L-796568 free base can be used for the research of obesity.
For research use only. We do not sell to patients.
- CAS No.: 211031-01-5
- Formula: C31H27F3N4O3S2
- Molecular Weight:624.70
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Biological Activity
Description
L-796568 free base is a β(3)-adrenergic receptor agonist. L-796568 free base can be used for the research of obesity[1].
Cellular Effect
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
0.003 μM
Compound: 2
|
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
|
10.1016/s0960-894x(04)00462-7 |
| CHO | EC50 |
0.003 μM
Compound: 2
|
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
Agonist activity (EC50) was assessed by measuring cAMP levels in CHO cells expressing cloned human Beta-3 adrenergic receptor
|
[PMID: 15149682] |
| CHO | EC50 |
0.003 μM
Compound: 3, L-796568
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Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP production
Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP production
|
[PMID: 17632003] |
| CHO | EC50 |
0.43 nM
Compound: 3; MK-0634
|
Agonist activity at rhesus monkey beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
Agonist activity at rhesus monkey beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
|
[PMID: 26709102] |
| CHO | EC50 |
17 nM
Compound: 3; MK-0634
|
Agonist activity at rhesus monkey beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serum
Agonist activity at rhesus monkey beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serum
|
[PMID: 26709102] |
| CHO | EC50 |
2 nM
Compound: 3; MK-0634
|
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
|
[PMID: 26709102] |
| CHO | EC50 |
2400 nM
Compound: 2e
|
In vitro functional efficacy in stimulating increase in cAMP in chinese hamster ovary (CHO) cells expressing the cloned human beta-2 receptor.
In vitro functional efficacy in stimulating increase in cAMP in chinese hamster ovary (CHO) cells expressing the cloned human beta-2 receptor.
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[PMID: 11052788] |
| CHO | EC50 |
25 nM
Compound: 3; MK-0634
|
Agonist activity at dog beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
Agonist activity at dog beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
|
[PMID: 26709102] |
| CHO | EC50 |
3.6 nM
Compound: 1
|
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
Agonistic activity at human beta3 adrenergic receptor expressed in CHO cells assessed as amount of cAMP released after 1 hr by fluorescence resonance energy transfer immuno assay
|
[PMID: 20181479] |
| CHO | EC50 |
3.6 nM
Compound: 2e
|
In vitro functional efficacy as increased cAMP in chinese hamster ovary (CHO) cells expressing human beta-3 receptor
In vitro functional efficacy as increased cAMP in chinese hamster ovary (CHO) cells expressing human beta-3 receptor
|
[PMID: 11052788] |
| CHO | EC50 |
3400 nM
Compound: 3; MK-0634
|
Agonist activity at rat beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
Agonist activity at rat beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay
|
[PMID: 26709102] |
| CHO | EC50 |
4800 nM
Compound: 2e
|
In vitro functional efficacy in stimulating increase in cAMP in chinese hamster ovary (CHO) cells expressing the cloned human beta-1 receptor.
In vitro functional efficacy in stimulating increase in cAMP in chinese hamster ovary (CHO) cells expressing the cloned human beta-1 receptor.
|
[PMID: 11052788] |
| CHO | EC50 |
7.9 nM
Compound: 3; MK-0634
|
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serum
Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as accumulation of cAMP after 30 mins by TR-FRET assay in presence of 40% serum
|
[PMID: 26709102] |
| CHO | IC50 |
2.3 μM
Compound: 1
|
Displacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
Displacement of [125I]cyanopindolol from human beta 1 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
|
[PMID: 20181479] |
| CHO | IC50 |
2.3 μM
Compound: 1
|
Displacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
Displacement of [125I]cyanopindolol from human beta 2 adrenergic receptor expressed in CHO cells at 10 uM after 3 to 4 hrs by scintillation counter
|
[PMID: 20181479] |
| CHO | IC50 |
2300 nM
Compound: 2e
|
Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-1 adrenergic receptor in the presence of [125I]- iodocyanopindolol.
Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-1 adrenergic receptor in the presence of [125I]- iodocyanopindolol.
|
[PMID: 11052788] |
| CHO | IC50 |
2300 nM
Compound: 2e
|
Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-2 adrenergic receptor in the presence of [125I]- iodocyanopindolol.
Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-2 adrenergic receptor in the presence of [125I]- iodocyanopindolol.
|
[PMID: 11052788] |
| CHO | IC50 |
46 nM
Compound: 2e
|
Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]- iodocyanopindolol.
Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]- iodocyanopindolol.
|
[PMID: 11052788] |
| HEK293 | IC50 |
5 μM
Compound: 3; MK-0634
|
Inhibition of human SERT expressed in HEK293 cells preincubated for 30 mins followed by fluorescent substrate addition measured after 30 mins by plate reader analysis
Inhibition of human SERT expressed in HEK293 cells preincubated for 30 mins followed by fluorescent substrate addition measured after 30 mins by plate reader analysis
|
[PMID: 26709102] |
Chemical Information
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CAS No. 211031-01-5
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Molecular Weight 624.70
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Formula C31H27F3N4O3S2
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SMILES
O=S(C1=CC=C(C=C1)C2=NC(C3=CC=C(C=C3)C(F)(F)F)=CS2)(NC4=CC=C(C=C4)CCNC[C@@H](C5=CC=CN=C5)O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
Select Batch:
Purity:
99.98%
Assay:
99.98%
ee.:
99.98%
References
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L-796568 free base Related Classifications
HY-19401A Related Classifications
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